Domain-selective targeting of BET proteins in cancer and immunological diseases

Cancer and inflammation are strongly interconnected processes. Chronic inflammatory pathologies can be at the heart of tumor development; similarly, tumor-elicited inflammation is a consequence of many cancers. The mechanistic interdependence between cancer and inflammatory pathologies points toward...

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Published inCurrent opinion in chemical biology Vol. 57; pp. 184 - 193
Main Authors Petretich, Massimo, Demont, Emmanuel H., Grandi, Paola
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 01.08.2020
Subjects
Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
BD1
BD2
BET
Bromodomain
Cancer
Chemical probes
Drug Discovery
Humans
Immune System Diseases - drug therapy
Immune System Diseases - metabolism
Immunologic Factors - chemistry
Immunologic Factors - pharmacology
Inflammation
Inflammation - drug therapy
Inflammation - metabolism
Molecular Targeted Therapy
Neoplasms - drug therapy
Neoplasms - metabolism
ProTAC
Protein Domains - drug effects
Proteins - antagonists & inhibitors
Proteins - metabolism
Selectivity
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
BET
BD2
ProTAC
Selectivity
Inflammation
Bromodomain
Chemical probes
BD1
Cancer
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Abstract Cancer and inflammation are strongly interconnected processes. Chronic inflammatory pathologies can be at the heart of tumor development; similarly, tumor-elicited inflammation is a consequence of many cancers. The mechanistic interdependence between cancer and inflammatory pathologies points toward common protein effectors which represent potential shared targets for pharmacological intervention. Epigenetic mechanisms often drive resistance to cancer therapy and immunomodulatory strategies. The bromodomain and extraterminal domain (BET) proteins are epigenetic adapters which play a major role in controlling cell proliferation and the production of inflammatory mediators. A plethora of small molecules aimed at inhibiting BET protein function to treat cancer and inflammatory diseases have populated academic and industry efforts in the last 10 years. In this review, we will discuss recent pharmacological approaches aimed at targeting a single or a subset of the eight bromodomains within the BET family which have the potential to tease apart clinical efficacy and safety signals of BET inhibitors.
AbstractList Cancer and inflammation are strongly interconnected processes. Chronic inflammatory pathologies can be at the heart of tumor development; similarly, tumor-elicited inflammation is a consequence of many cancers. The mechanistic interdependence between cancer and inflammatory pathologies points toward common protein effectors which represent potential shared targets for pharmacological intervention. Epigenetic mechanisms often drive resistance to cancer therapy and immunomodulatory strategies. The bromodomain and extraterminal domain (BET) proteins are epigenetic adapters which play a major role in controlling cell proliferation and the production of inflammatory mediators. A plethora of small molecules aimed at inhibiting BET protein function to treat cancer and inflammatory diseases have populated academic and industry efforts in the last 10 years. In this review, we will discuss recent pharmacological approaches aimed at targeting a single or a subset of the eight bromodomains within the BET family which have the potential to tease apart clinical efficacy and safety signals of BET inhibitors.
Author Demont, Emmanuel H.
Petretich, Massimo
Grandi, Paola
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/32741705$$D View this record in MEDLINE/PubMed
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Cites_doi 10.1038/cdd.2014.124
10.1038/nature09589
10.1016/j.jmgm.2018.03.005
10.1006/geno.1997.5000
10.1021/acs.jmedchem.7b01666
10.1158/1535-7163.MCT-18-1129
10.1242/dev.004481
10.1016/j.bmcl.2012.02.041
10.3390/ijms17111849
10.1016/j.molcel.2018.11.006
10.1172/JCI120633
10.1073/pnas.1422165112
10.1038/onc.2013.179
10.1038/nchembio.2329
10.1038/s41467-017-02403-5
10.1128/MCB.23.15.5354-5365.2003
10.1158/1541-7786.MCR-15-0472
10.1073/pnas.1310658110
10.1021/acs.jmedchem.6b00070
10.1016/j.cell.2012.02.013
10.1038/nchembio.2210
10.1021/acs.jmedchem.7b00275
10.1021/acs.jmedchem.0c00614
10.1101/sqb.2017.82.033829
10.1021/acschembio.5b00216
10.1021/jm300346w
10.1371/journal.pone.0083190
10.1038/nchembio.2209
10.1021/acs.jmedchem.0c00796
10.1016/j.molcel.2017.02.027
10.1038/s41594-019-0309-8
10.1021/acs.jmedchem.0c00566
10.1038/emboj.2012.233
10.1038/nature10334
10.1126/science.1249830
10.1021/acschembio.0c00058
10.1038/nature09504
10.1042/BJ20090928
10.1016/j.cell.2015.11.062
10.1038/ncomms6418
10.1073/pnas.1700109114
10.1021/acs.jmedchem.0c00628
10.1016/j.ccr.2014.01.028
10.1038/ncomms13855
10.1016/j.chembiol.2014.05.009
10.1021/acs.jmedchem.9b01010
10.1038/ng.480
10.1016/j.bbrc.2016.06.021
10.1038/nri2634
10.1016/j.bbagrm.2009.03.005
10.1016/j.celrep.2019.08.051
10.1124/mol.117.110379
10.1016/j.ejmech.2018.04.006
10.1038/s41586-020-1930-8
10.1093/annonc/mdx157
10.1021/jm200108t
10.1016/j.celrep.2017.12.078
10.1126/science.aaz8455
10.1371/journal.pone.0023656
10.1101/gad.331231.119
10.1021/acsmedchemlett.0c00247
10.1038/nature10509
10.1038/nchembio.1197
10.1021/jm401334s
10.4049/jimmunol.1202838
10.1093/nar/gku449
10.1038/nature14898
10.1038/nrc3659
10.4049/jimmunol.0803917
10.1182/blood-2014-10-607309
10.1021/acs.jmedchem.5b01135
10.1126/science.aal2066
10.1073/pnas.1615601114
10.1016/j.tips.2011.12.002
10.1016/j.ejmech.2019.111633
10.1016/j.clim.2018.02.013
10.1128/MCB.01341-10
10.1021/acs.jmedchem.0c00605
10.1158/1078-0432.CCR-12-3904
10.1186/gb-2013-14-2-r18
10.1073/pnas.1102140108
10.1021/acs.jmedchem.5b01708
10.1038/s41589-018-0055-y
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Keywords BET
BD2
ProTAC
Selectivity
Inflammation
Bromodomain
Chemical probes
BD1
Cancer
Language English
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References Chung (bib16) 2011; 54
Bao (bib47) 2017; 114
Zaware, Zhou (bib29) 2019; 26
Lee (bib46) 2017; 8
Garcia-Gomez, Rodriguez-Ubreva, Ballestar (bib4) 2018; 196
Gacias (bib52) 2014; 21
Zuber (bib6) 2011; 478
Marcotte (bib10) 2016; 164
Kim (bib37) 2019; 33
Pivot-Pajot (bib43) 2003; 23
Lamonica (bib44) 2011; 108
Jahagirdar (bib61) 2017; 92
Zhang (bib74) 2019; 18
Law (bib56) 2018; 61
Olp (bib78) 2020; 15
French (bib11) 2014; 14
Liu (bib65) 2018; 151
Medzhitov, Horng (bib1) 2009; 9
Gadd (bib71) 2017; 13
Jones, Numata, Shimane (bib42) 1997; 45
Kockmann (bib50) 2013; 14
Zou (bib19) 2014; 33
Doroshow, Eder, LoRusso (bib25) 2017; 28
Tyler (bib33) 2017; 356
Chen (bib57) 2019; 182
Waring (bib75) 2016; 12
Itzen (bib32) 2014; 42
Taniguchi (bib5) 2016; 17
Bunnage, Chekler, Jones (bib51) 2013; 9
Miller (bib31) 2016; 7
Zengerle, Chan, Ciulli (bib70) 2015; 10
Wells (bib2) 2009; 182
Baratta (bib7) 2015; 112
Faivre (bib66) 2020 578
Shi (bib18) 2014; 25
Kharenko (bib60) 2016; 477
Baud (bib69) 2014; 346
Filippakopoulos (bib14) 2010; 468
Zhang (bib53) 2013; 56
Ouyang (bib64) 2017; 60
Liu (bib45) 2014; 21
Baud (bib55) 2016; 59
Jiang (bib67) 2019; 62
Dawson (bib22) 2011; 478
Nowak (bib72) 2018; 14
Filippakopoulos (bib49) 2012; 149
Rathert (bib48) 2015; 525
Blake (bib73) 2019; 79
Tanaka (bib77) 2016; 12
Nicodeme (bib9) 2010; 468
Gaucher (bib26) 2012; 31
Seal (bib68) 2012; 22
Bradbury (bib76) 2016; 59
Picaud (bib58) 2013; 110
Prinjha, Witherington, Lee (bib13) 2012; 33
Greally (bib3) 2018; 14
Cheung (bib54) 2017; 114
Mahdi (bib12) 2009; 41
Vidler (bib17) 2012; 55
Shimamura (bib23) 2013; 19
Rahman (bib30) 2011; 31
Li (bib38) 2018; 22
Raux (bib62) 2016; 59
Wang (bib41) 2009; 425
Asangani (bib21) 2016; 14
Belkina, Nikolajczyk, Denis (bib8) 2013; 190
Wessel (bib36) 2019; 28
Lambert (bib20) 2019; 73
Shang (bib27) 2007; 134
Niu (bib63) 2019; 129
Velisek (bib40) 2011; 6
Hsu, Blobel (bib34) 2017; 82
Hsu (bib35) 2017; 66
Bharatham (bib15) 2018; 81
Stonestrom (bib28) 2015; 125
Gyuris (bib39) 2009; 1789
Park-Min (bib24) 2014; 5
McLure (bib59) 2013; 8
Stonestrom (10.1016/j.cbpa.2020.02.003_bib28) 2015; 125
Hsu (10.1016/j.cbpa.2020.02.003_bib34) 2017; 82
Preston (10.1016/j.cbpa.2020.02.003_sref83) 2020; 11
Liu (10.1016/j.cbpa.2020.02.003_bib45) 2014; 21
Shimamura (10.1016/j.cbpa.2020.02.003_bib23) 2013; 19
Gilan (10.1016/j.cbpa.2020.02.003_bib80) 2020; 368
Kockmann (10.1016/j.cbpa.2020.02.003_bib50) 2013; 14
Belkina (10.1016/j.cbpa.2020.02.003_bib8) 2013; 190
Zengerle (10.1016/j.cbpa.2020.02.003_bib70) 2015; 10
Zhang (10.1016/j.cbpa.2020.02.003_bib53) 2013; 56
Ouyang (10.1016/j.cbpa.2020.02.003_bib64) 2017; 60
Pivot-Pajot (10.1016/j.cbpa.2020.02.003_bib43) 2003; 23
Tanaka (10.1016/j.cbpa.2020.02.003_sref77) 2016; 12
Picaud (10.1016/j.cbpa.2020.02.003_bib58) 2013; 110
Jiang (10.1016/j.cbpa.2020.02.003_sref67) 2019; 62
Zaware (10.1016/j.cbpa.2020.02.003_bib29) 2019; 26
Bradbury (10.1016/j.cbpa.2020.02.003_bib76) 2016; 59
Mahdi (10.1016/j.cbpa.2020.02.003_bib12) 2009; 41
Taniguchi (10.1016/j.cbpa.2020.02.003_bib5) 2016; 17
Baud (10.1016/j.cbpa.2020.02.003_bib55) 2016; 59
Baratta (10.1016/j.cbpa.2020.02.003_sref7) 2015; 112
Marcotte (10.1016/j.cbpa.2020.02.003_bib10) 2016; 164
Bunnage (10.1016/j.cbpa.2020.02.003_bib51) 2013; 9
Wessel (10.1016/j.cbpa.2020.02.003_bib36) 2019; 28
Waring (10.1016/j.cbpa.2020.02.003_sref75) 2016; 12
Gaucher (10.1016/j.cbpa.2020.02.003_bib26) 2012; 31
Gadd (10.1016/j.cbpa.2020.02.003_bib71) 2017; 13
Niu (10.1016/j.cbpa.2020.02.003_bib63) 2019; 129
Seal (10.1016/j.cbpa.2020.02.003_bib82) 2020; 63
Lee (10.1016/j.cbpa.2020.02.003_bib46) 2017; 8
Bao (10.1016/j.cbpa.2020.02.003_sref47) 2017; 114
Zou (10.1016/j.cbpa.2020.02.003_bib19) 2014; 33
Zuber (10.1016/j.cbpa.2020.02.003_bib6) 2011; 478
Rahman (10.1016/j.cbpa.2020.02.003_bib30) 2011; 31
McLure (10.1016/j.cbpa.2020.02.003_bib59) 2013; 8
Zhang (10.1016/j.cbpa.2020.02.003_bib74) 2019; 18
Kim (10.1016/j.cbpa.2020.02.003_bib37) 2019; 33
Seal (10.1016/j.cbpa.2020.02.003_bib68) 2012; 22
Dawson (10.1016/j.cbpa.2020.02.003_bib22) 2011; 478
Raux (10.1016/j.cbpa.2020.02.003_bib62) 2016; 59
Greally (10.1016/j.cbpa.2020.02.003_bib3) 2018; 14
Rathert (10.1016/j.cbpa.2020.02.003_bib48) 2015; 525
Baud (10.1016/j.cbpa.2020.02.003_bib69) 2014; 346
Chung (10.1016/j.cbpa.2020.02.003_bib16) 2011; 54
Lambert (10.1016/j.cbpa.2020.02.003_bib20) 2019; 73
Faivre (10.1016/j.cbpa.2020.02.003_sref66) 2020
Garcia-Gomez (10.1016/j.cbpa.2020.02.003_bib4) 2018; 196
Nicodeme (10.1016/j.cbpa.2020.02.003_bib9) 2010; 468
Wang (10.1016/j.cbpa.2020.02.003_bib41) 2009; 425
Cheung (10.1016/j.cbpa.2020.02.003_bib54) 2017; 114
Tyler (10.1016/j.cbpa.2020.02.003_sref33) 2017; 356
Li (10.1016/j.cbpa.2020.02.003_bib38) 2018; 22
Olp (10.1016/j.cbpa.2020.02.003_sref78) 2020; 15
Gyuris (10.1016/j.cbpa.2020.02.003_bib39) 2009; 1789
Wells (10.1016/j.cbpa.2020.02.003_bib2) 2009; 182
Lamonica (10.1016/j.cbpa.2020.02.003_bib44) 2011; 108
Watson (10.1016/j.cbpa.2020.02.003_sref85) 2020; 63
Wellaway (10.1016/j.cbpa.2020.02.003_bib84) 2020; 63
Doroshow (10.1016/j.cbpa.2020.02.003_bib25) 2017; 28
Velisek (10.1016/j.cbpa.2020.02.003_bib40) 2011; 6
Shi (10.1016/j.cbpa.2020.02.003_bib18) 2014; 25
Law (10.1016/j.cbpa.2020.02.003_bib56) 2018; 61
French (10.1016/j.cbpa.2020.02.003_bib11) 2014; 14
Itzen (10.1016/j.cbpa.2020.02.003_bib32) 2014; 42
Asangani (10.1016/j.cbpa.2020.02.003_bib21) 2016; 14
Bharatham (10.1016/j.cbpa.2020.02.003_bib15) 2018; 81
Nowak (10.1016/j.cbpa.2020.02.003_sref72) 2018; 14
Preston (10.1016/j.cbpa.2020.02.003_bib81) 2020; 63
Hsu (10.1016/j.cbpa.2020.02.003_bib35) 2017; 66
Medzhitov (10.1016/j.cbpa.2020.02.003_bib1) 2009; 9
Vidler (10.1016/j.cbpa.2020.02.003_bib17) 2012; 55
Chen (10.1016/j.cbpa.2020.02.003_bib57) 2019; 182
Kharenko (10.1016/j.cbpa.2020.02.003_bib60) 2016; 477
Filippakopoulos (10.1016/j.cbpa.2020.02.003_bib49) 2012; 149
Blake (10.1016/j.cbpa.2020.02.003_bib73) 2019; 79
Jones (10.1016/j.cbpa.2020.02.003_bib42) 1997; 45
Gacias (10.1016/j.cbpa.2020.02.003_bib52) 2014; 21
Shang (10.1016/j.cbpa.2020.02.003_bib27) 2007; 134
Miller (10.1016/j.cbpa.2020.02.003_bib31) 2016; 7
Sheppard (10.1016/j.cbpa.2020.02.003_sref79) 2020; 63
Filippakopoulos (10.1016/j.cbpa.2020.02.003_bib14) 2010; 468
Park-Min (10.1016/j.cbpa.2020.02.003_bib24) 2014; 5
Liu (10.1016/j.cbpa.2020.02.003_bib65) 2018; 151
Jahagirdar (10.1016/j.cbpa.2020.02.003_bib61) 2017; 92
Prinjha (10.1016/j.cbpa.2020.02.003_bib13) 2012; 33
References_xml – volume: 346
  start-page: 638
  year: 2014
  ident: bib69
  article-title: A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
  publication-title: Science
  contributor:
    fullname: Baud
– volume: 12
  start-page: 1089
  year: 2016
  ident: bib77
  article-title: Design and characterization of bivalent BET inhibitors
  publication-title: Nat Chem Biol
  contributor:
    fullname: Tanaka
– volume: 54
  start-page: 3827
  year: 2011
  end-page: 3838
  ident: bib16
  article-title: Discovery and characterization of small molecule inhibitors of the BET family bromodomains
  publication-title: J Med Chem
  contributor:
    fullname: Chung
– volume: 22
  start-page: 796
  year: 2018
  end-page: 808
  ident: bib38
  article-title: BRD4 promotes DNA repair and mediates the formation of TMPRSS2-ERG gene rearrangements in prostate cancer
  publication-title: Cell Rep
  contributor:
    fullname: Li
– volume: 14
  start-page: 149
  year: 2014
  end-page: 150
  ident: bib11
  article-title: NUT midline carcinoma
  publication-title: Nat Rev Canc
  contributor:
    fullname: French
– volume: 17
  year: 2016
  ident: bib5
  article-title: The bromodomain and extra-terminal domain (BET) family: functional anatomy of BET paralogous proteins
  publication-title: Int J Mol Sci
  contributor:
    fullname: Taniguchi
– volume: 14
  start-page: 706
  year: 2018
  end-page: 714
  ident: bib72
  article-title: Plasticity in binding confers selectivity in ligand-induced protein degradation
  publication-title: Nat Chem Biol
  contributor:
    fullname: Nowak
– volume: 55
  start-page: 7346
  year: 2012
  end-page: 7359
  ident: bib17
  article-title: Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
  publication-title: J Med Chem
  contributor:
    fullname: Vidler
– volume: 129
  start-page: 3361
  year: 2019
  end-page: 3373
  ident: bib63
  article-title: Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV
  publication-title: J Clin Invest
  contributor:
    fullname: Niu
– volume: 468
  start-page: 1067
  year: 2010
  ident: bib14
  article-title: Selective inhibition of BET bromodomains
  publication-title: Nature
  contributor:
    fullname: Filippakopoulos
– volume: 33
  start-page: 146
  year: 2012
  end-page: 153
  ident: bib13
  article-title: Place your BETs: the therapeutic potential of bromodomains
  publication-title: Trends Pharmacol Sci
  contributor:
    fullname: Lee
– volume: 182
  start-page: 111633
  year: 2019
  ident: bib57
  article-title: Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins
  publication-title: Eur J Med Chem
  contributor:
    fullname: Chen
– volume: 60
  start-page: 9990
  year: 2017
  end-page: 10012
  ident: bib64
  article-title: Discovery of a small-molecule bromodomain-containing protein 4 (BRD4) inhibitor that induces AMP-activated protein kinase-modulated autophagy-associated cell death in breast cancer
  publication-title: J Med Chem
  contributor:
    fullname: Ouyang
– volume: 9
  start-page: 195
  year: 2013
  ident: bib51
  article-title: Target validation using chemical probes
  publication-title: Nat Chem Biol
  contributor:
    fullname: Jones
– volume: 14
  start-page: 324
  year: 2016
  end-page: 331
  ident: bib21
  article-title: BET bromodomain inhibitors enhance efficacy and disrupt resistance to AR antagonists in the treatment of prostate cancer
  publication-title: Mol Canc Res
  contributor:
    fullname: Asangani
– volume: 45
  start-page: 529
  year: 1997
  end-page: 534
  ident: bib42
  article-title: Identification and characterization of BRDT: a testis-specific gene related to the bromodomain genes RING3 and Drosophila fsh
  publication-title: Genomics
  contributor:
    fullname: Shimane
– volume: 19
  start-page: 6183
  year: 2013
  end-page: 6192
  ident: bib23
  article-title: Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer
  publication-title: Clin Canc Res
  contributor:
    fullname: Shimamura
– volume: 59
  start-page: 1492
  year: 2016
  end-page: 1500
  ident: bib55
  article-title: New synthetic routes to triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective Bromo and extra-terminal (BET) bromodomain inhibition
  publication-title: J Med Chem
  contributor:
    fullname: Baud
– volume: 62
  start-page: 11080
  year: 2019
  end-page: 11107
  ident: bib67
  article-title: Discovery of benzo[cd]indol-2(1H)-ones and pyrrolo[4,3,2-de]quinolin-2(1H)-ones as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the first bromodomain with potential high efficiency against acute gouty arthritis
  publication-title: J Med Chem
  contributor:
    fullname: Jiang
– volume: 112
  start-page: 232
  year: 2015
  end-page: 237
  ident: bib7
  article-title: An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma
  publication-title: Proc Natl Acad Sci U S A
  contributor:
    fullname: Baratta
– volume: 61
  start-page: 4317
  year: 2018
  end-page: 4334
  ident: bib56
  article-title: Discovery of tetrahydroquinoxalines as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the second bromodomain
  publication-title: J Med Chem
  contributor:
    fullname: Law
– volume: 79
  year: 2019
  ident: bib73
  article-title: Abstract 4452: GNE-0011, a novel monovalent BRD4 degrader
  publication-title: Am Assoc Cancer Res
  contributor:
    fullname: Blake
– volume: 73
  start-page: 621
  year: 2019
  end-page: 638 e17
  ident: bib20
  article-title: Interactome rewiring following pharmacological targeting of BET bromodomains
  publication-title: Mol Cell
  contributor:
    fullname: Lambert
– volume: 59
  start-page: 1634
  year: 2016
  end-page: 1641
  ident: bib62
  article-title: Exploring selective inhibition of the first bromodomain of the human bromodomain and extra-terminal domain (BET) proteins
  publication-title: J Med Chem
  contributor:
    fullname: Raux
– volume: 164
  start-page: 293
  year: 2016
  end-page: 309
  ident: bib10
  article-title: Functional genomic landscape of human breast cancer drivers, vulnerabilities, and resistance
  publication-title: Cell
  contributor:
    fullname: Marcotte
– volume: 108
  start-page: E159
  year: 2011
  end-page: E168
  ident: bib44
  article-title: Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes
  publication-title: Proc Natl Acad Sci U S A
  contributor:
    fullname: Lamonica
– volume: 23
  start-page: 5354
  year: 2003
  end-page: 5365
  ident: bib43
  article-title: Acetylation-dependent chromatin reorganization by BRDT, a testis-specific bromodomain-containing protein
  publication-title: Mol Cell Biol
  contributor:
    fullname: Pivot-Pajot
– volume: 9
  start-page: 692
  year: 2009
  end-page: 703
  ident: bib1
  article-title: Transcriptional control of the inflammatory response
  publication-title: Nat Rev Immunol
  contributor:
    fullname: Horng
– volume: 182
  start-page: 7331
  year: 2009
  end-page: 7341
  ident: bib2
  article-title: New insights into the molecular basis of T cell anergy: anergy factors, avoidance sensors, and epigenetic imprinting
  publication-title: J Immunol
  contributor:
    fullname: Wells
– volume: 6
  start-page: e23656
  year: 2011
  ident: bib40
  article-title: GABAergic neuron deficit as an idiopathic generalized epilepsy mechanism: the role of BRD2 haploinsufficiency in juvenile myoclonic epilepsy
  publication-title: PloS One
  contributor:
    fullname: Velisek
– volume: 477
  start-page: 62
  year: 2016
  end-page: 67
  ident: bib60
  article-title: RVX-297- a novel BD2 selective inhibitor of BET bromodomains
  publication-title: Biochem Biophys Res Commun
  contributor:
    fullname: Kharenko
– volume: 12
  start-page: 1097
  year: 2016
  ident: bib75
  article-title: Potent and selective bivalent inhibitors of BET bromodomains
  publication-title: Nat Chem Biol
  contributor:
    fullname: Waring
– volume: 10
  start-page: 1770
  year: 2015
  end-page: 1777
  ident: bib70
  article-title: Selective small molecule induced degradation of the BET bromodomain protein BRD4
  publication-title: ACS Chem Biol
  contributor:
    fullname: Ciulli
– volume: 56
  start-page: 9251
  year: 2013
  end-page: 9264
  ident: bib53
  article-title: Structure-Guided design of potent diazobenzene inhibitors for the BET bromodomains
  publication-title: J Med Chem
  contributor:
    fullname: Zhang
– volume: 478
  start-page: 529
  year: 2011
  ident: bib22
  article-title: Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
  publication-title: Nature
  contributor:
    fullname: Dawson
– volume: 28
  start-page: 1776
  year: 2017
  end-page: 1787
  ident: bib25
  article-title: BET inhibitors: a novel epigenetic approach
  publication-title: Ann Oncol
  contributor:
    fullname: LoRusso
– volume: 14
  year: 2018
  ident: bib3
  article-title: Cancer epigenetics: moving forward
  publication-title: PLoS Genet
  contributor:
    fullname: Greally
– volume: 33
  start-page: 1751
  year: 2019
  end-page: 1774
  ident: bib37
  article-title: Systematic bromodomain protein screens identify homologous recombination and R-loop suppression pathways involved in genome integrity
  publication-title: Genes Dev
  contributor:
    fullname: Kim
– volume: 114
  start-page: E3993
  year: 2017
  end-page: E4001
  ident: bib47
  article-title: Brd4 modulates the innate immune response through Mnk2-eIF4E pathway-dependent translational control of IkappaBalpha
  publication-title: Proc Natl Acad Sci U S A
  contributor:
    fullname: Bao
– volume: 42
  start-page: 7577
  year: 2014
  end-page: 7590
  ident: bib32
  article-title: Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation
  publication-title: Nucleic Acids Res
  contributor:
    fullname: Itzen
– volume: 8
  start-page: 2217
  year: 2017
  ident: bib46
  article-title: Brd4 binds to active enhancers to control cell identity gene induction in adipogenesis and myogenesis
  publication-title: Nat Commun
  contributor:
    fullname: Lee
– volume: 81
  start-page: 197
  year: 2018
  end-page: 210
  ident: bib15
  article-title: The role of ZA channel water-mediated interactions in the design of bromodomain-selective BET inhibitors
  publication-title: J Mol Graph Model
  contributor:
    fullname: Bharatham
– volume: 125
  start-page: 2825
  year: 2015
  end-page: 2834
  ident: bib28
  article-title: Functions of BET proteins in erythroid gene expression
  publication-title: Blood
  contributor:
    fullname: Stonestrom
– volume: 1789
  start-page: 413
  year: 2009
  end-page: 421
  ident: bib39
  article-title: The chromatin-targeting protein Brd2 is required for neural tube closure and embryogenesis
  publication-title: Biochim Biophys Acta
  contributor:
    fullname: Gyuris
– volume: 425
  start-page: 71
  year: 2009
  end-page: 83
  ident: bib41
  article-title: Brd2 disruption in mice causes severe obesity without Type 2 diabetes
  publication-title: Biochem J
  contributor:
    fullname: Wang
– volume: 8
  start-page: e83190
  year: 2013
  ident: bib59
  article-title: RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist
  publication-title: PloS One
  contributor:
    fullname: McLure
– volume: 190
  start-page: 3670
  year: 2013
  ident: bib8
  article-title: BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses
  publication-title: J Immunol
  contributor:
    fullname: Denis
– volume: 25
  start-page: 210
  year: 2014
  end-page: 225
  ident: bib18
  article-title: Disrupting the interaction of BRD4 with diacetylated Twist suppresses tumorigenesis in basal-like breast cancer
  publication-title: Canc Cell
  contributor:
    fullname: Shi
– volume: 151
  start-page: 450
  year: 2018
  end-page: 461
  ident: bib65
  article-title: Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation
  publication-title: Eur J Med Chem
  contributor:
    fullname: Liu
– volume: 7
  start-page: 13855
  year: 2016
  ident: bib31
  article-title: A bromodomain–DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT
  publication-title: Nat Commun
  contributor:
    fullname: Miller
– volume: 14
  start-page: R18
  year: 2013
  ident: bib50
  article-title: The BET protein FSH functionally interacts with ASH1 to orchestrate global gene activity in Drosophila
  publication-title: Genome Biol
  contributor:
    fullname: Kockmann
– volume: 114
  start-page: 2952
  year: 2017
  ident: bib54
  article-title: BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice
  publication-title: Proc Natl Acad Sci Unit States Am
  contributor:
    fullname: Cheung
– volume: 15
  start-page: 1036
  year: 2020
  end-page: 1049
  ident: bib78
  article-title: Covalent-fragment screening of Brd4 Identifies a ligandable SiteOrthogonal to the acetyl-lysine binding sites
  publication-title: ACS Chem. Biol
  contributor:
    fullname: Olp
– volume: 41
  start-page: 1319
  year: 2009
  end-page: 1324
  ident: bib12
  article-title: Specific interaction between genotype, smoking and autoimmunity to citrullinated alpha-enolase in the etiology of rheumatoid arthritis
  publication-title: Nat Genet
  contributor:
    fullname: Mahdi
– volume: 196
  start-page: 64
  year: 2018
  end-page: 71
  ident: bib4
  article-title: Epigenetic interplay between immune, stromal and cancer cells in the tumor microenvironment
  publication-title: Clin Immunol
  contributor:
    fullname: Ballestar
– volume: 66
  start-page: 102
  year: 2017
  end-page: 116 e7
  ident: bib35
  article-title: The BET protein BRD2 cooperates with CTCF to enforce transcriptional and architectural boundaries
  publication-title: Mol Cell
  contributor:
    fullname: Hsu
– volume: 110
  start-page: 19754
  year: 2013
  ident: bib58
  article-title: RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
  publication-title: Proc Natl Acad Sci Unit States Am
  contributor:
    fullname: Picaud
– volume: 356
  start-page: 1397
  year: 2017
  end-page: 1401
  ident: bib33
  article-title: Click chemistry enables preclinical evaluation of targeted epigenetic therapies
  publication-title: Science
  contributor:
    fullname: Tyler
– volume: 21
  start-page: 1950
  year: 2014
  end-page: 1960
  ident: bib45
  article-title: BRD4 regulates Nanog expression in mouse embryonic stem cells and preimplantation embryos
  publication-title: Cell Death Differ
  contributor:
    fullname: Liu
– volume: 22
  start-page: 2968
  year: 2012
  end-page: 2972
  ident: bib68
  article-title: Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)
  publication-title: Bioorg Med Chem Lett
  contributor:
    fullname: Seal
– volume: 468
  start-page: 1119
  year: 2010
  ident: bib9
  article-title: Suppression of inflammation by a synthetic histone mimic
  publication-title: Nature
  contributor:
    fullname: Nicodeme
– volume: 31
  start-page: 3809
  year: 2012
  end-page: 3820
  ident: bib26
  article-title: Bromodomain-dependent stage-specific male genome programming by Brdt
  publication-title: EMBO J
  contributor:
    fullname: Gaucher
– volume: 149
  start-page: 214
  year: 2012
  end-page: 231
  ident: bib49
  article-title: Histone recognition and large-scale structural analysis of the human bromodomain family
  publication-title: Cell
  contributor:
    fullname: Filippakopoulos
– volume: 92
  start-page: 694
  year: 2017
  ident: bib61
  article-title: RVX-297, a BET bromodomain inhibitor, has therapeutic effects in preclinical models of acute inflammation and autoimmune disease
  publication-title: Mol Pharmacol
  contributor:
    fullname: Jahagirdar
– volume: 28
  start-page: 3497
  year: 2019
  end-page: 3509 e4
  ident: bib36
  article-title: Functional analysis of the replication fork proteome identifies BET proteins as PCNA regulators
  publication-title: Cell Rep
  contributor:
    fullname: Wessel
– volume: 18
  start-page: 1302
  year: 2019
  end-page: 1311
  ident: bib74
  article-title: Acquired resistance to BET-PROTACs (Proteolysis-Targeting chimeras) caused by genomic alterations in core components of E3 ligase complexes
  publication-title: Mol Canc Therapeut
  contributor:
    fullname: Zhang
– volume: 478
  start-page: 524
  year: 2011
  ident: bib6
  article-title: RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
  publication-title: Nature
  contributor:
    fullname: Zuber
– volume: 82
  start-page: 37
  year: 2017
  end-page: 43
  ident: bib34
  article-title: The role of bromodomain and extraterminal motif (BET) proteins in chromatin structure
  publication-title: Cold Spring Harbor Symp Quant Biol
  contributor:
    fullname: Blobel
– volume: 21
  start-page: 841
  year: 2014
  end-page: 854
  ident: bib52
  article-title: Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression
  publication-title: Chem Biol
  contributor:
    fullname: Gacias
– volume: 134
  start-page: 3507
  year: 2007
  end-page: 3515
  ident: bib27
  article-title: The first bromodomain of Brdt, a testis-specific member of the BET sub-family of double-bromodomain-containing proteins, is essential for male germ cell differentiation
  publication-title: Development
  contributor:
    fullname: Shang
– volume: 26
  start-page: 870
  year: 2019
  end-page: 879
  ident: bib29
  article-title: Bromodomain biology and drug discovery
  publication-title: Nat Struct Mol Biol
  contributor:
    fullname: Zhou
– volume: 59
  start-page: 7801
  year: 2016
  end-page: 7817
  ident: bib76
  article-title: Optimization of a series of bivalent triazolopyridazine based bromodomain and extraterminal inhibitors: the discovery of (3r)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phen oxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
  publication-title: J Med Chem
  contributor:
    fullname: Bradbury
– volume: 31
  start-page: 2641
  year: 2011
  end-page: 2652
  ident: bib30
  article-title: The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3
  publication-title: Mol Cell Biol
  contributor:
    fullname: Rahman
– volume: 5
  start-page: 5418
  year: 2014
  ident: bib24
  article-title: Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation
  publication-title: Nat Commun
  contributor:
    fullname: Park-Min
– volume: 13
  start-page: 514
  year: 2017
  end-page: 521
  ident: bib71
  article-title: Structural basis of PROTAC cooperative recognition for selective protein degradation
  publication-title: Nat Chem Biol
  contributor:
    fullname: Gadd
– volume: 525
  start-page: 543
  year: 2015
  end-page: 547
  ident: bib48
  article-title: Transcriptional plasticity promotes primary and acquired resistance to BET inhibition
  publication-title: Nature
  contributor:
    fullname: Rathert
– start-page: 306
  year: 2020 578
  end-page: 310
  ident: bib66
  article-title: Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
  publication-title: Nature
  contributor:
    fullname: Faivre
– volume: 33
  start-page: 2395
  year: 2014
  end-page: 2404
  ident: bib19
  article-title: Brd4 maintains constitutively active NF-kappaB in cancer cells by binding to acetylated RelA
  publication-title: Oncogene
  contributor:
    fullname: Zou
– volume: 21
  start-page: 1950
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib45
  article-title: BRD4 regulates Nanog expression in mouse embryonic stem cells and preimplantation embryos
  publication-title: Cell Death Differ
  doi: 10.1038/cdd.2014.124
  contributor:
    fullname: Liu
– volume: 14
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib3
  article-title: Cancer epigenetics: moving forward
  publication-title: PLoS Genet
  contributor:
    fullname: Greally
– volume: 468
  start-page: 1119
  year: 2010
  ident: 10.1016/j.cbpa.2020.02.003_bib9
  article-title: Suppression of inflammation by a synthetic histone mimic
  publication-title: Nature
  doi: 10.1038/nature09589
  contributor:
    fullname: Nicodeme
– volume: 81
  start-page: 197
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib15
  article-title: The role of ZA channel water-mediated interactions in the design of bromodomain-selective BET inhibitors
  publication-title: J Mol Graph Model
  doi: 10.1016/j.jmgm.2018.03.005
  contributor:
    fullname: Bharatham
– volume: 45
  start-page: 529
  year: 1997
  ident: 10.1016/j.cbpa.2020.02.003_bib42
  article-title: Identification and characterization of BRDT: a testis-specific gene related to the bromodomain genes RING3 and Drosophila fsh
  publication-title: Genomics
  doi: 10.1006/geno.1997.5000
  contributor:
    fullname: Jones
– volume: 61
  start-page: 4317
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib56
  article-title: Discovery of tetrahydroquinoxalines as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the second bromodomain
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.7b01666
  contributor:
    fullname: Law
– volume: 18
  start-page: 1302
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib74
  article-title: Acquired resistance to BET-PROTACs (Proteolysis-Targeting chimeras) caused by genomic alterations in core components of E3 ligase complexes
  publication-title: Mol Canc Therapeut
  doi: 10.1158/1535-7163.MCT-18-1129
  contributor:
    fullname: Zhang
– volume: 134
  start-page: 3507
  year: 2007
  ident: 10.1016/j.cbpa.2020.02.003_bib27
  article-title: The first bromodomain of Brdt, a testis-specific member of the BET sub-family of double-bromodomain-containing proteins, is essential for male germ cell differentiation
  publication-title: Development
  doi: 10.1242/dev.004481
  contributor:
    fullname: Shang
– volume: 22
  start-page: 2968
  year: 2012
  ident: 10.1016/j.cbpa.2020.02.003_bib68
  article-title: Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)
  publication-title: Bioorg Med Chem Lett
  doi: 10.1016/j.bmcl.2012.02.041
  contributor:
    fullname: Seal
– volume: 17
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib5
  article-title: The bromodomain and extra-terminal domain (BET) family: functional anatomy of BET paralogous proteins
  publication-title: Int J Mol Sci
  doi: 10.3390/ijms17111849
  contributor:
    fullname: Taniguchi
– volume: 73
  start-page: 621
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib20
  article-title: Interactome rewiring following pharmacological targeting of BET bromodomains
  publication-title: Mol Cell
  doi: 10.1016/j.molcel.2018.11.006
  contributor:
    fullname: Lambert
– volume: 129
  start-page: 3361
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib63
  article-title: Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV
  publication-title: J Clin Invest
  doi: 10.1172/JCI120633
  contributor:
    fullname: Niu
– volume: 112
  start-page: 232
  year: 2015
  ident: 10.1016/j.cbpa.2020.02.003_sref7
  article-title: An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma
  publication-title: Proc Natl Acad Sci U S A
  doi: 10.1073/pnas.1422165112
  contributor:
    fullname: Baratta
– volume: 33
  start-page: 2395
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib19
  article-title: Brd4 maintains constitutively active NF-kappaB in cancer cells by binding to acetylated RelA
  publication-title: Oncogene
  doi: 10.1038/onc.2013.179
  contributor:
    fullname: Zou
– volume: 13
  start-page: 514
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib71
  article-title: Structural basis of PROTAC cooperative recognition for selective protein degradation
  publication-title: Nat Chem Biol
  doi: 10.1038/nchembio.2329
  contributor:
    fullname: Gadd
– volume: 8
  start-page: 2217
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib46
  article-title: Brd4 binds to active enhancers to control cell identity gene induction in adipogenesis and myogenesis
  publication-title: Nat Commun
  doi: 10.1038/s41467-017-02403-5
  contributor:
    fullname: Lee
– volume: 23
  start-page: 5354
  year: 2003
  ident: 10.1016/j.cbpa.2020.02.003_bib43
  article-title: Acetylation-dependent chromatin reorganization by BRDT, a testis-specific bromodomain-containing protein
  publication-title: Mol Cell Biol
  doi: 10.1128/MCB.23.15.5354-5365.2003
  contributor:
    fullname: Pivot-Pajot
– volume: 14
  start-page: 324
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib21
  article-title: BET bromodomain inhibitors enhance efficacy and disrupt resistance to AR antagonists in the treatment of prostate cancer
  publication-title: Mol Canc Res
  doi: 10.1158/1541-7786.MCR-15-0472
  contributor:
    fullname: Asangani
– volume: 110
  start-page: 19754
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib58
  article-title: RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
  publication-title: Proc Natl Acad Sci Unit States Am
  doi: 10.1073/pnas.1310658110
  contributor:
    fullname: Picaud
– volume: 59
  start-page: 7801
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib76
  article-title: Optimization of a series of bivalent triazolopyridazine based bromodomain and extraterminal inhibitors: the discovery of (3r)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phen oxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.6b00070
  contributor:
    fullname: Bradbury
– volume: 149
  start-page: 214
  year: 2012
  ident: 10.1016/j.cbpa.2020.02.003_bib49
  article-title: Histone recognition and large-scale structural analysis of the human bromodomain family
  publication-title: Cell
  doi: 10.1016/j.cell.2012.02.013
  contributor:
    fullname: Filippakopoulos
– volume: 12
  start-page: 1097
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_sref75
  article-title: Potent and selective bivalent inhibitors of BET bromodomains
  publication-title: Nat Chem Biol
  doi: 10.1038/nchembio.2210
  contributor:
    fullname: Waring
– volume: 60
  start-page: 9990
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib64
  article-title: Discovery of a small-molecule bromodomain-containing protein 4 (BRD4) inhibitor that induces AMP-activated protein kinase-modulated autophagy-associated cell death in breast cancer
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.7b00275
  contributor:
    fullname: Ouyang
– volume: 63
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_sref85
  article-title: GSK789: a selective inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) proteins
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.0c00614
  contributor:
    fullname: Watson
– volume: 82
  start-page: 37
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib34
  article-title: The role of bromodomain and extraterminal motif (BET) proteins in chromatin structure
  publication-title: Cold Spring Harbor Symp Quant Biol
  doi: 10.1101/sqb.2017.82.033829
  contributor:
    fullname: Hsu
– volume: 10
  start-page: 1770
  year: 2015
  ident: 10.1016/j.cbpa.2020.02.003_bib70
  article-title: Selective small molecule induced degradation of the BET bromodomain protein BRD4
  publication-title: ACS Chem Biol
  doi: 10.1021/acschembio.5b00216
  contributor:
    fullname: Zengerle
– volume: 55
  start-page: 7346
  year: 2012
  ident: 10.1016/j.cbpa.2020.02.003_bib17
  article-title: Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
  publication-title: J Med Chem
  doi: 10.1021/jm300346w
  contributor:
    fullname: Vidler
– volume: 8
  start-page: e83190
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib59
  article-title: RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist
  publication-title: PloS One
  doi: 10.1371/journal.pone.0083190
  contributor:
    fullname: McLure
– volume: 12
  start-page: 1089
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_sref77
  article-title: Design and characterization of bivalent BET inhibitors
  publication-title: Nat Chem Biol
  doi: 10.1038/nchembio.2209
  contributor:
    fullname: Tanaka
– volume: 63
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_bib82
  article-title: The optimisation of a novel, weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a potent and selective Second Bromodomain (BD2) inhibitor
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.0c00796
  contributor:
    fullname: Seal
– volume: 66
  start-page: 102
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib35
  article-title: The BET protein BRD2 cooperates with CTCF to enforce transcriptional and architectural boundaries
  publication-title: Mol Cell
  doi: 10.1016/j.molcel.2017.02.027
  contributor:
    fullname: Hsu
– volume: 26
  start-page: 870
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib29
  article-title: Bromodomain biology and drug discovery
  publication-title: Nat Struct Mol Biol
  doi: 10.1038/s41594-019-0309-8
  contributor:
    fullname: Zaware
– volume: 63
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_bib84
  article-title: Structure-based design of a Bromodomain and Extraterminal Domain (BET) inhibitor selective for the N-terminal Bromodomains that retains an anti-inflammatory and anti-proliferative phenotype
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.0c00566
  contributor:
    fullname: Wellaway
– volume: 31
  start-page: 3809
  year: 2012
  ident: 10.1016/j.cbpa.2020.02.003_bib26
  article-title: Bromodomain-dependent stage-specific male genome programming by Brdt
  publication-title: EMBO J
  doi: 10.1038/emboj.2012.233
  contributor:
    fullname: Gaucher
– volume: 478
  start-page: 524
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib6
  article-title: RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
  publication-title: Nature
  doi: 10.1038/nature10334
  contributor:
    fullname: Zuber
– volume: 346
  start-page: 638
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib69
  article-title: A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
  publication-title: Science
  doi: 10.1126/science.1249830
  contributor:
    fullname: Baud
– volume: 15
  start-page: 1036
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_sref78
  article-title: Covalent-fragment screening of Brd4 Identifies a ligandable SiteOrthogonal to the acetyl-lysine binding sites
  publication-title: ACS Chem. Biol
  doi: 10.1021/acschembio.0c00058
  contributor:
    fullname: Olp
– volume: 468
  start-page: 1067
  year: 2010
  ident: 10.1016/j.cbpa.2020.02.003_bib14
  article-title: Selective inhibition of BET bromodomains
  publication-title: Nature
  doi: 10.1038/nature09504
  contributor:
    fullname: Filippakopoulos
– volume: 425
  start-page: 71
  year: 2009
  ident: 10.1016/j.cbpa.2020.02.003_bib41
  article-title: Brd2 disruption in mice causes severe obesity without Type 2 diabetes
  publication-title: Biochem J
  doi: 10.1042/BJ20090928
  contributor:
    fullname: Wang
– volume: 164
  start-page: 293
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib10
  article-title: Functional genomic landscape of human breast cancer drivers, vulnerabilities, and resistance
  publication-title: Cell
  doi: 10.1016/j.cell.2015.11.062
  contributor:
    fullname: Marcotte
– volume: 5
  start-page: 5418
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib24
  article-title: Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation
  publication-title: Nat Commun
  doi: 10.1038/ncomms6418
  contributor:
    fullname: Park-Min
– volume: 114
  start-page: E3993
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_sref47
  article-title: Brd4 modulates the innate immune response through Mnk2-eIF4E pathway-dependent translational control of IkappaBalpha
  publication-title: Proc Natl Acad Sci U S A
  doi: 10.1073/pnas.1700109114
  contributor:
    fullname: Bao
– volume: 63
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_sref79
  article-title: Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.0c00628
  contributor:
    fullname: Sheppard
– volume: 25
  start-page: 210
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib18
  article-title: Disrupting the interaction of BRD4 with diacetylated Twist suppresses tumorigenesis in basal-like breast cancer
  publication-title: Canc Cell
  doi: 10.1016/j.ccr.2014.01.028
  contributor:
    fullname: Shi
– volume: 7
  start-page: 13855
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib31
  article-title: A bromodomain–DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT
  publication-title: Nat Commun
  doi: 10.1038/ncomms13855
  contributor:
    fullname: Miller
– volume: 21
  start-page: 841
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib52
  article-title: Selective chemical modulation of gene transcription favors oligodendrocyte lineage progression
  publication-title: Chem Biol
  doi: 10.1016/j.chembiol.2014.05.009
  contributor:
    fullname: Gacias
– volume: 62
  start-page: 11080
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_sref67
  article-title: Discovery of benzo[cd]indol-2(1H)-ones and pyrrolo[4,3,2-de]quinolin-2(1H)-ones as bromodomain and extra-terminal domain (BET) inhibitors with selectivity for the first bromodomain with potential high efficiency against acute gouty arthritis
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.9b01010
  contributor:
    fullname: Jiang
– volume: 41
  start-page: 1319
  year: 2009
  ident: 10.1016/j.cbpa.2020.02.003_bib12
  article-title: Specific interaction between genotype, smoking and autoimmunity to citrullinated alpha-enolase in the etiology of rheumatoid arthritis
  publication-title: Nat Genet
  doi: 10.1038/ng.480
  contributor:
    fullname: Mahdi
– volume: 477
  start-page: 62
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib60
  article-title: RVX-297- a novel BD2 selective inhibitor of BET bromodomains
  publication-title: Biochem Biophys Res Commun
  doi: 10.1016/j.bbrc.2016.06.021
  contributor:
    fullname: Kharenko
– volume: 9
  start-page: 692
  year: 2009
  ident: 10.1016/j.cbpa.2020.02.003_bib1
  article-title: Transcriptional control of the inflammatory response
  publication-title: Nat Rev Immunol
  doi: 10.1038/nri2634
  contributor:
    fullname: Medzhitov
– volume: 1789
  start-page: 413
  year: 2009
  ident: 10.1016/j.cbpa.2020.02.003_bib39
  article-title: The chromatin-targeting protein Brd2 is required for neural tube closure and embryogenesis
  publication-title: Biochim Biophys Acta
  doi: 10.1016/j.bbagrm.2009.03.005
  contributor:
    fullname: Gyuris
– volume: 28
  start-page: 3497
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib36
  article-title: Functional analysis of the replication fork proteome identifies BET proteins as PCNA regulators
  publication-title: Cell Rep
  doi: 10.1016/j.celrep.2019.08.051
  contributor:
    fullname: Wessel
– volume: 92
  start-page: 694
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib61
  article-title: RVX-297, a BET bromodomain inhibitor, has therapeutic effects in preclinical models of acute inflammation and autoimmune disease
  publication-title: Mol Pharmacol
  doi: 10.1124/mol.117.110379
  contributor:
    fullname: Jahagirdar
– volume: 151
  start-page: 450
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib65
  article-title: Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation
  publication-title: Eur J Med Chem
  doi: 10.1016/j.ejmech.2018.04.006
  contributor:
    fullname: Liu
– start-page: 306
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_sref66
  article-title: Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
  publication-title: Nature
  doi: 10.1038/s41586-020-1930-8
  contributor:
    fullname: Faivre
– volume: 28
  start-page: 1776
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib25
  article-title: BET inhibitors: a novel epigenetic approach
  publication-title: Ann Oncol
  doi: 10.1093/annonc/mdx157
  contributor:
    fullname: Doroshow
– volume: 54
  start-page: 3827
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib16
  article-title: Discovery and characterization of small molecule inhibitors of the BET family bromodomains
  publication-title: J Med Chem
  doi: 10.1021/jm200108t
  contributor:
    fullname: Chung
– volume: 22
  start-page: 796
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib38
  article-title: BRD4 promotes DNA repair and mediates the formation of TMPRSS2-ERG gene rearrangements in prostate cancer
  publication-title: Cell Rep
  doi: 10.1016/j.celrep.2017.12.078
  contributor:
    fullname: Li
– volume: 368
  start-page: 387
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_bib80
  article-title: Selective targetting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
  publication-title: Science
  doi: 10.1126/science.aaz8455
  contributor:
    fullname: Gilan
– volume: 79
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib73
  article-title: Abstract 4452: GNE-0011, a novel monovalent BRD4 degrader
  publication-title: Am Assoc Cancer Res
  contributor:
    fullname: Blake
– volume: 6
  start-page: e23656
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib40
  article-title: GABAergic neuron deficit as an idiopathic generalized epilepsy mechanism: the role of BRD2 haploinsufficiency in juvenile myoclonic epilepsy
  publication-title: PloS One
  doi: 10.1371/journal.pone.0023656
  contributor:
    fullname: Velisek
– volume: 33
  start-page: 1751
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib37
  article-title: Systematic bromodomain protein screens identify homologous recombination and R-loop suppression pathways involved in genome integrity
  publication-title: Genes Dev
  doi: 10.1101/gad.331231.119
  contributor:
    fullname: Kim
– volume: 11
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_sref83
  article-title: GSK973 is an inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) family
  publication-title: ACS Med Chem Lett
  doi: 10.1021/acsmedchemlett.0c00247
  contributor:
    fullname: Preston
– volume: 478
  start-page: 529
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib22
  article-title: Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
  publication-title: Nature
  doi: 10.1038/nature10509
  contributor:
    fullname: Dawson
– volume: 9
  start-page: 195
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib51
  article-title: Target validation using chemical probes
  publication-title: Nat Chem Biol
  doi: 10.1038/nchembio.1197
  contributor:
    fullname: Bunnage
– volume: 56
  start-page: 9251
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib53
  article-title: Structure-Guided design of potent diazobenzene inhibitors for the BET bromodomains
  publication-title: J Med Chem
  doi: 10.1021/jm401334s
  contributor:
    fullname: Zhang
– volume: 190
  start-page: 3670
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib8
  article-title: BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses
  publication-title: J Immunol
  doi: 10.4049/jimmunol.1202838
  contributor:
    fullname: Belkina
– volume: 42
  start-page: 7577
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib32
  article-title: Brd4 activates P-TEFb for RNA polymerase II CTD phosphorylation
  publication-title: Nucleic Acids Res
  doi: 10.1093/nar/gku449
  contributor:
    fullname: Itzen
– volume: 525
  start-page: 543
  year: 2015
  ident: 10.1016/j.cbpa.2020.02.003_bib48
  article-title: Transcriptional plasticity promotes primary and acquired resistance to BET inhibition
  publication-title: Nature
  doi: 10.1038/nature14898
  contributor:
    fullname: Rathert
– volume: 14
  start-page: 149
  year: 2014
  ident: 10.1016/j.cbpa.2020.02.003_bib11
  article-title: NUT midline carcinoma
  publication-title: Nat Rev Canc
  doi: 10.1038/nrc3659
  contributor:
    fullname: French
– volume: 182
  start-page: 7331
  year: 2009
  ident: 10.1016/j.cbpa.2020.02.003_bib2
  article-title: New insights into the molecular basis of T cell anergy: anergy factors, avoidance sensors, and epigenetic imprinting
  publication-title: J Immunol
  doi: 10.4049/jimmunol.0803917
  contributor:
    fullname: Wells
– volume: 125
  start-page: 2825
  year: 2015
  ident: 10.1016/j.cbpa.2020.02.003_bib28
  article-title: Functions of BET proteins in erythroid gene expression
  publication-title: Blood
  doi: 10.1182/blood-2014-10-607309
  contributor:
    fullname: Stonestrom
– volume: 59
  start-page: 1492
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib55
  article-title: New synthetic routes to triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective Bromo and extra-terminal (BET) bromodomain inhibition
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.5b01135
  contributor:
    fullname: Baud
– volume: 356
  start-page: 1397
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_sref33
  article-title: Click chemistry enables preclinical evaluation of targeted epigenetic therapies
  publication-title: Science
  doi: 10.1126/science.aal2066
  contributor:
    fullname: Tyler
– volume: 114
  start-page: 2952
  year: 2017
  ident: 10.1016/j.cbpa.2020.02.003_bib54
  article-title: BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice
  publication-title: Proc Natl Acad Sci Unit States Am
  doi: 10.1073/pnas.1615601114
  contributor:
    fullname: Cheung
– volume: 33
  start-page: 146
  year: 2012
  ident: 10.1016/j.cbpa.2020.02.003_bib13
  article-title: Place your BETs: the therapeutic potential of bromodomains
  publication-title: Trends Pharmacol Sci
  doi: 10.1016/j.tips.2011.12.002
  contributor:
    fullname: Prinjha
– volume: 182
  start-page: 111633
  year: 2019
  ident: 10.1016/j.cbpa.2020.02.003_bib57
  article-title: Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins
  publication-title: Eur J Med Chem
  doi: 10.1016/j.ejmech.2019.111633
  contributor:
    fullname: Chen
– volume: 196
  start-page: 64
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_bib4
  article-title: Epigenetic interplay between immune, stromal and cancer cells in the tumor microenvironment
  publication-title: Clin Immunol
  doi: 10.1016/j.clim.2018.02.013
  contributor:
    fullname: Garcia-Gomez
– volume: 31
  start-page: 2641
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib30
  article-title: The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3
  publication-title: Mol Cell Biol
  doi: 10.1128/MCB.01341-10
  contributor:
    fullname: Rahman
– volume: 63
  year: 2020
  ident: 10.1016/j.cbpa.2020.02.003_bib81
  article-title: The design and synthesis of a highly selective and in vivo capable inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) family of proteins
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.0c00605
  contributor:
    fullname: Preston
– volume: 19
  start-page: 6183
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib23
  article-title: Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer
  publication-title: Clin Canc Res
  doi: 10.1158/1078-0432.CCR-12-3904
  contributor:
    fullname: Shimamura
– volume: 14
  start-page: R18
  year: 2013
  ident: 10.1016/j.cbpa.2020.02.003_bib50
  article-title: The BET protein FSH functionally interacts with ASH1 to orchestrate global gene activity in Drosophila
  publication-title: Genome Biol
  doi: 10.1186/gb-2013-14-2-r18
  contributor:
    fullname: Kockmann
– volume: 108
  start-page: E159
  year: 2011
  ident: 10.1016/j.cbpa.2020.02.003_bib44
  article-title: Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes
  publication-title: Proc Natl Acad Sci U S A
  doi: 10.1073/pnas.1102140108
  contributor:
    fullname: Lamonica
– volume: 59
  start-page: 1634
  year: 2016
  ident: 10.1016/j.cbpa.2020.02.003_bib62
  article-title: Exploring selective inhibition of the first bromodomain of the human bromodomain and extra-terminal domain (BET) proteins
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.5b01708
  contributor:
    fullname: Raux
– volume: 14
  start-page: 706
  year: 2018
  ident: 10.1016/j.cbpa.2020.02.003_sref72
  article-title: Plasticity in binding confers selectivity in ligand-induced protein degradation
  publication-title: Nat Chem Biol
  doi: 10.1038/s41589-018-0055-y
  contributor:
    fullname: Nowak
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Snippet Cancer and inflammation are strongly interconnected processes. Chronic inflammatory pathologies can be at the heart of tumor development; similarly,...
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SubjectTerms Animals
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
BD1
BD2
BET
Bromodomain
Cancer
Chemical probes
Drug Discovery
Humans
Immune System Diseases - drug therapy
Immune System Diseases - metabolism
Immunologic Factors - chemistry
Immunologic Factors - pharmacology
Inflammation
Inflammation - drug therapy
Inflammation - metabolism
Molecular Targeted Therapy
Neoplasms - drug therapy
Neoplasms - metabolism
ProTAC
Protein Domains - drug effects
Proteins - antagonists & inhibitors
Proteins - metabolism
Selectivity
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
Title Domain-selective targeting of BET proteins in cancer and immunological diseases
URI https://dx.doi.org/10.1016/j.cbpa.2020.02.003
https://www.ncbi.nlm.nih.gov/pubmed/32741705
https://search.proquest.com/docview/2430093881
Volume 57
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