The PROTAC technology in drug development

Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to...

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Published inCell biochemistry and function Vol. 37; no. 1; pp. 21 - 30
Main Authors Zou, Yutian, Ma, Danhui, Wang, Yinyin
Format Journal Article
LanguageEnglish
Published England Wiley Subscription Services, Inc 01.01.2019
John Wiley and Sons Inc
Subjects
Biodegradation
cancer
Drug development
Drug Development - methods
Humans
New technology
PROTAC
Proteasome Endopeptidase Complex - metabolism
protein degradation
Proteins
Proteolysis
Recombinant Fusion Proteins - metabolism
Review
small molecule
Ubiquitin
Ubiquitin-protein ligase
Ubiquitin-Protein Ligases - metabolism
Ubiquitination
drug development
small molecule
cancer
PROTAC
protein degradation
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Abstract Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. Significance of the study This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.
AbstractList Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. SIGNIFICANCE OF THE STUDY: This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC.Significance of the studyThis review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. SIGNIFICANCE OF THE STUDY: This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. SIGNIFICANCE OF THE STUDY: This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.
Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. Significance of the study This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.
Author Zou, Yutian
Wang, Yinyin
Ma, Danhui
AuthorAffiliation 1 The State Laboratory of Membrane Biology, Department of Basic Medicine, School of Medicine Tsinghua University Beijing China
2 Department of Science Brookwood High School Snellville Georgia
AuthorAffiliation_xml – name: 1 The State Laboratory of Membrane Biology, Department of Basic Medicine, School of Medicine Tsinghua University Beijing China
– name: 2 Department of Science Brookwood High School Snellville Georgia
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  fullname: Ma, Danhui
  organization: Tsinghua University
– sequence: 3
  givenname: Yinyin
  orcidid: 0000-0003-1285-0507
  surname: Wang
  fullname: Wang, Yinyin
  email: wangyinyin@mail.tsinghua.edu.cn
  organization: Tsinghua University
BackLink https://www.ncbi.nlm.nih.gov/pubmed/30604499$$D View this record in MEDLINE/PubMed
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Cites_doi 10.1126/science.aab1433
10.1016/j.ejmech.2018.01.063
10.1016/j.bioorg.2018.09.005
10.2174/1568009616666151112122502
10.1111/cas.13198
10.1016/j.chembiol.2015.05.009
10.1016/S1097-2765(00)00074-5
10.1021/acs.jmedchem.6b01781
10.1016/j.bmc.2011.03.057
10.1021/acs.jmedchem.6b01816
10.1016/j.chembiol.2017.10.011
10.1038/nrd.2016.211
10.1021/acscentsci.6b00280
10.1007/s10555-017-9698-5
10.1016/j.bmcl.2016.09.041
10.1021/acschembio.7b00985
10.1074/mcp.T300009-MCP200
10.1021/acschembio.5b00442
10.1126/science.aam7340
10.1038/leu.2016.393
10.1038/onc.2008.320
10.1038/s41375-018-0044-x
10.1016/j.febslet.2011.03.019
10.1016/j.ejmech.2018.03.071
10.1038/nn.3637
10.1021/acs.jmedchem.7b01333
10.1021/acs.jmedchem.6b01872
10.1007/978-1-4939-3127-9_42
10.1158/2159-8290.CD-NB2018-015
10.1038/s41589-018-0010-y
10.1016/j.ejmech.2018.03.066
10.1016/S0076-6879(05)99054-X
10.1021/acs.jmedchem.8b00506
10.1073/pnas.1803662115
10.1016/j.bmcl.2005.04.008
10.1203/PDR.0b013e3181d35017
10.1016/j.bmcl.2008.07.114
10.1124/mol.116.105569
10.1016/j.bbrc.2018.02.096
10.1016/j.bbrc.2014.10.006
10.1111/cas.12272
10.3390/molecules23081958
10.1038/leu.2017.207
10.2174/1386207043328364
10.1016/j.bmcl.2003.11.042
10.1124/mol.107.040840
10.1016/j.cellsig.2007.11.010
10.1002/anie.201507634
10.1073/pnas.1521738113
10.1021/cb8001792
10.1016/j.cbpa.2016.06.031
10.1016/S0960-894X(00)00208-0
10.1038/nchembio.597
10.1016/S0960-894X(99)00185-7
10.1038/s41422-018-0055-1
10.1021/ja100691p
10.1016/j.cbpa.2017.05.016
10.1002/bies.201700247
10.1021/ja039025z
10.1002/anie.201507978
10.1002/cbic.200700438
10.1039/C7CC03879H
10.1038/nbt.1608
10.1038/aja.2008.26
10.1021/jacs.8b05807
10.1038/nchembio.1858
10.1074/jbc.M116.768853
10.1021/acs.jmedchem.7b00635
10.1021/acsmedchemlett.8b00106
10.1016/j.chembiol.2016.02.016
10.1038/s42003-018-0105-8
10.1021/acschembio.5b00216
10.1016/j.biocel.2018.06.001
10.1021/acs.jmedchem.7b01655
10.1016/j.bmcl.2018.05.057
10.1002/tcr.201800032
10.1016/j.ebiom.2018.09.005
10.1042/EBC20170030
10.1016/j.bcp.2016.07.017
10.1016/j.bone.2018.03.027
10.1038/nchembio.2538
10.1002/psc.2858
10.1016/j.cell.2018.02.030
10.1146/annurev-pharmtox-010715-103507
10.1016/j.chembiol.2017.05.024
10.1016/j.pharmthera.2017.02.027
10.1016/j.bmc.2011.09.041
10.1016/j.bbrc.2018.09.169
10.1016/j.chembiol.2017.10.005
10.1186/s13045-016-0362-2
10.1073/pnas.141230798
10.1002/j.1460-2075.1992.tb05307.x
10.1016/j.bioorg.2018.08.028
10.1016/j.chembiol.2017.09.009
10.1016/S1097-2765(00)80156-2
10.1038/cddis.2014.471
10.1021/acschembio.6b01068
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ISSN 0263-6484
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IsDoiOpenAccess true
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Issue 1
Keywords drug development
small molecule
cancer
PROTAC
protein degradation
Language English
License Attribution
2019 The Authors Cell Biochemistry and Function Published by John Wiley & Sons Ltd.
This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
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OpenAccessLink https://proxy.k.utb.cz/login?url=https://onlinelibrary.wiley.com/doi/abs/10.1002%2Fcbf.3369
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References 2004; 126
2000; 6
2004; 7
2018; 81
2016; 1366
2018; 40
2008; 3
2015; 348
2008; 73
2017; 355
1992; 11
2011; 19
2014; 453
2016; 33
2010; 67
2009; 11
2017; 31
2018; 9
2018; 8
2014; 5
2018; 173
2017; 36
2017; 39
2018; 1
2010; 28
2000; 10
2018; 497
2008; 27
2003; 2
2007; 8
2016; 113
2016; 116
2014; 17
2008; 20
2018; 32
2001; 98
2017; 61
2018; 28
2018; 140
2005; 399
2018; 146
2008; 18
2018; 101
2013; 104
2017; 24
2015; 11
2015; 10
2017; 292
2005
2017; 174
2018; 505
2018; 61
2016; 16
2011; 7
2018; 25
1999; 9
2016; 55
2017; 108
2017; 53
2017; 91
2018; 151
2016; 2
2017; 16
2004; 14
2018; 112
2015; 22
2017; 57
2018; 115
2017; 12
2010; 132
2018
1998; 2
2005; 15
2016; 26
2011; 585
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e_1_2_9_75_1
e_1_2_9_98_1
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e_1_2_9_56_1
e_1_2_9_33_1
e_1_2_9_90_1
e_1_2_9_71_1
e_1_2_9_14_1
e_1_2_9_37_1
e_1_2_9_18_1
e_1_2_9_41_1
e_1_2_9_64_1
e_1_2_9_87_1
e_1_2_9_22_1
e_1_2_9_45_1
e_1_2_9_68_1
e_1_2_9_83_1
e_1_2_9_6_1
e_1_2_9_60_1
e_1_2_9_2_1
e_1_2_9_26_1
e_1_2_9_49_1
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e_1_2_9_99_1
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e_1_2_9_11_1
e_1_2_9_34_1
e_1_2_9_57_1
e_1_2_9_95_1
e_1_2_9_76_1
e_1_2_9_91_1
Caruso C (e_1_2_9_97_1) 2018; 8
e_1_2_9_15_1
e_1_2_9_38_1
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e_1_2_9_96_1
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e_1_2_9_39_1
e_1_2_9_16_1
e_1_2_9_58_1
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References_xml – volume: 355
  start-page: 1163
  issue: 6330
  year: 2017
  end-page: 1167
  article-title: Waste disposal—an attractive strategy for cancer therapy
  publication-title: Science
– volume: 505
  start-page: 542
  issue: 2
  year: 2018
  end-page: 547
  article-title: Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)
  publication-title: Biochem Biophys Res Commun
– volume: 61
  start-page: 6685
  issue: 15
  year: 2018
  end-page: 6704
  article-title: Discovery of QCA570 as an exceptionally potent and efficacious proteolysis targeting chimera (PROTAC) degrader of the Bromodomain and extra‐terminal (BET) proteins capable of inducing complete and durable tumor regression
  publication-title: J Med Chem
– volume: 10
  start-page: 1770
  issue: 8
  year: 2015
  end-page: 1777
  article-title: Selective small molecule induced degradation of the BET bromodomain protein BRD4
  publication-title: ACS Chem Biol
– year: 2005
– volume: 33
  start-page: 186
  year: 2016
  end-page: 194
  article-title: Chemical genetics approaches for selective intervention in epigenetics
  publication-title: Curr Opin Chem Biol
– volume: 23
  start-page: 453
  issue: 4
  year: 2016
  end-page: 461
  article-title: Specific knockdown of endogenous tau protein by peptide‐directed ubiquitin‐proteasome degradation
  publication-title: Cell Chem Biol
– volume: 115
  start-page: E7285
  issue: 31
  year: 2018
  end-page: E7292
  article-title: Delineating the role of cooperativity in the design of potent PROTACs for BTK
  publication-title: Proc Natl Acad Sci U S a
– volume: 1
  start-page: 100
  issue: 1
  year: 2018
  article-title: Androgen receptor degradation by the proteolysis‐targeting chimera ARCC‐4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
  publication-title: Commun Biol
– volume: 6
  start-page: 751
  issue: 3
  year: 2000
  end-page: 756
  article-title: Harnessing the ubiquitination machinery to target the degradation of specific cellular proteins
  publication-title: Mol Cell
– volume: 7
  start-page: 538
  issue: 8
  year: 2011
  end-page: 543
  article-title: Small‐molecule hydrophobic tagging‐induced degradation of HaloTag fusion proteins
  publication-title: Nat Chem Biol
– volume: 10
  start-page: 1303
  issue: 11
  year: 2000
  end-page: 1306
  article-title: Synthesis and evaluation of geldanamycin‐testosterone hybrids
  publication-title: Bioorg Med Chem Lett
– volume: 14
  start-page: 645
  issue: 3
  year: 2004
  end-page: 648
  article-title: Degradation of target protein in living cells by small‐molecule proteolysis inducer
  publication-title: Bioorg Med Chem Lett
– volume: 116
  start-page: 200
  year: 2016
  end-page: 209
  article-title: New strategy for renal fibrosis: targeting Smad3 proteins for ubiquitination and degradation
  publication-title: Biochem Pharmacol
– volume: 292
  start-page: 4556
  issue: 11
  year: 2017
  end-page: 4570
  article-title: In vivo knockdown of pathogenic proteins via specific and nongenetic inhibitor of apoptosis protein (IAP)‐dependent protein erasers (SNIPERs)
  publication-title: J Biol Chem
– volume: 585
  start-page: 1147
  issue: 8
  year: 2011
  end-page: 1152
  article-title: Specific degradation of CRABP‐II via cIAP1‐mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein
  publication-title: FEBS Lett
– volume: 14
  start-page: 163
  issue: 2
  year: 2018
  end-page: 170
  article-title: Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation
  publication-title: Nat Chem Biol
– volume: 399
  start-page: 833
  year: 2005
  end-page: 847
  article-title: Chimeric molecules to target proteins for ubiquitination and degradation
  publication-title: Methods Enzymol
– volume: 81
  start-page: 373
  year: 2018
  end-page: 381
  article-title: Discovery of Wogonin‐based PROTACs against CDK9 and capable of achieving antitumor activity
  publication-title: Bioorg Chem
– volume: 40
  issue: 4
  year: 2018
  article-title: PROTACs: an emerging targeting technique for protein degradation in drug discovery
  publication-title: Bioessays
– volume: 11
  start-page: 119
  issue: 1
  year: 2009
  end-page: 126
  article-title: Chimeric molecules facilitate the degradation of androgen receptors and repress the growth of LNCaP cells
  publication-title: Asian J Androl
– volume: 25
  start-page: 67
  issue: 1
  year: 2018
  end-page: 77
  article-title: The advantages of targeted protein degradation over inhibition: an RTK case study
  publication-title: Cell Chem Biol
– volume: 1366
  start-page: 549
  year: 2016
  end-page: 560
  article-title: Molecular design, synthesis, and evaluation of SNIPER (ER) that induces proteasomal degradation of ERα
  publication-title: Methods Mol Biol
– volume: 61
  start-page: 583
  issue: 2
  year: 2018
  end-page: 598
  article-title: Identification and characterization of Von Hippel‐Lindau‐recruiting proteolysis targeting chimeras (PROTACs) of TANK‐binding kinase 1
  publication-title: J Med Chem
– volume: 19
  start-page: 6768
  issue: 22
  year: 2011
  end-page: 6778
  article-title: Design, synthesis and biological evaluation of nuclear receptor‐degradation inducers
  publication-title: Bioorg Med Chem
– volume: 24
  start-page: 1181
  issue: 9
  year: 2017
  end-page: 1190
  article-title: Targeted protein degradation: from chemical biology to drug discovery
  publication-title: Cell Chem Biol
– volume: 17
  start-page: 471
  issue: 3
  year: 2014
  end-page: 480
  article-title: Rapid and reversible knockdown of endogenous proteins by peptide‐directed lysosomal degradation
  publication-title: Nat Neurosci
– volume: 53
  start-page: 7577
  issue: 54
  year: 2017
  end-page: 7580
  article-title: Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)
  publication-title: Chem Commun (Camb)
– volume: 2
  start-page: 571
  issue: 5
  year: 1998
  end-page: 580
  article-title: Ubiquitination and degradation of the substrate recognition subunits of SCF ubiquitin‐protein ligases
  publication-title: Mol Cell
– volume: 22
  start-page: 755
  issue: 6
  year: 2015
  end-page: 763
  article-title: Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4
  publication-title: Chem Biol
– volume: 22
  start-page: 196
  issue: 4
  year: 2016
  end-page: 200
  article-title: Degradation of Akt using protein‐catalyzed capture agents
  publication-title: J Pept Sci
– volume: 140
  start-page: 9299
  issue: 29
  year: 2018
  end-page: 9313
  article-title: 3‐Fluoro‐4‐hydroxyprolines: synthesis, conformational analysis, and Stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation
  publication-title: J Am Chem Soc
– volume: 11
  start-page: 611
  issue: 8
  year: 2015
  end-page: 617
  article-title: Catalytic in vivo protein knockdown by small‐molecule PROTACs
  publication-title: Nat Chem Biol
– volume: 61
  start-page: 453
  issue: 2
  year: 2018
  end-page: 461
  article-title: A “click chemistry platform” for the rapid synthesis of bispecific molecules for inducing protein degradation
  publication-title: J Med Chem
– volume: 12
  start-page: 892
  issue: 4
  year: 2017
  end-page: 898
  article-title: Proteolysis‐targeting chimeras: induced protein degradation as a therapeutic strategy
  publication-title: ACS Chem Biol
– volume: 61
  start-page: 462
  issue: 2
  year: 2018
  end-page: 481
  article-title: Discovery of a small‐molecule degrader of bromodomain and extra‐terminal (BET) proteins with picomolar cellular potencies and capable of achieving tumor regression
  publication-title: J Med Chem
– volume: 39
  start-page: 46
  year: 2017
  end-page: 53
  article-title: Targeted protein knockdown using small molecule degraders
  publication-title: Curr Opin Chem Biol
– volume: 81
  start-page: 536
  year: 2018
  end-page: 544
  article-title: Chemically induced degradation of CK2 by proteolysis targeting chimeras based on a ubiquitin‐proteasome pathway
  publication-title: Bioorg Chem
– volume: 151
  start-page: 237
  year: 2018
  end-page: 247
  article-title: Phthalimide conjugations for the degradation of oncogenic PI3K
  publication-title: Eur J Med Chem
– volume: 25
  start-page: 30
  issue: 1
  year: 2018
  end-page: 35
  article-title: Small‐molecule kinase downregulators
  publication-title: Cell Chem Biol
– volume: 16
  start-page: 101
  issue: 2
  year: 2017
  end-page: 114
  article-title: Induced protein degradation: an emerging drug discovery paradigm
  publication-title: Nat Rev Drug Discov
– volume: 13
  start-page: 628
  issue: 3
  year: 2018
  end-page: 635
  article-title: Development of stabilized peptide‐based PROTACs against estrogen receptor alpha
  publication-title: ACS Chem Biol
– volume: 3
  start-page: 677
  issue: 11
  year: 2008
  end-page: 692
  article-title: Design and applications of bifunctional small molecules: why two heads are better than one
  publication-title: ACS Chem Biol
– volume: 10
  start-page: 1831
  issue: 8
  year: 2015
  end-page: 1837
  article-title: HaloPROTACS: use of small molecule PROTACs to induce degradation of HaloTag fusion proteins
  publication-title: ACS Chem Biol
– volume: 497
  start-page: 410
  issue: 1
  year: 2018
  end-page: 415
  article-title: Selective degradation of BET proteins with dBET1, a proteolysis‐targeting chimera, potently reduces pro‐inflammatory responses in lipopolysaccharide‐activated microglia
  publication-title: Biochem Biophys Res Commun
– volume: 67
  start-page: 505
  issue: 5
  year: 2010
  end-page: 508
  article-title: Protacs for treatment of cancer
  publication-title: Pediatr Res
– volume: 61
  start-page: 517
  issue: 5
  year: 2017
  end-page: 527
  article-title: Protein degradation: a validated therapeutic strategy with exciting prospects
  publication-title: Essays Biochem
– volume: 113
  start-page: 7124
  issue: 26
  year: 2016
  end-page: 7129
  article-title: PROTAC‐induced BET protein degradation as a therapy for castration‐resistant prostate cancer
  publication-title: Proc Natl Acad Sci U S a
– volume: 36
  start-page: 585
  issue: 4
  year: 2017
  end-page: 598
  article-title: Emerging small molecule approaches to enhance the antimyeloma benefit of proteasome inhibitors
  publication-title: Cancer Metastasis Rev
– volume: 104
  start-page: 1492
  issue: 11
  year: 2013
  end-page: 1498
  article-title: Development of hybrid small molecules that induce degradation of estrogen receptor‐alpha and necrotic cell death in breast cancer cells
  publication-title: Cancer Sci
– volume: 9
  start-page: 134
  issue: 1
  year: 2016
  article-title: Inhibition of bromodomain and extra‐terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell‐mediated cytotoxicity in multiple myeloma cells: role of cMYC‐IRF4‐miR‐125b interplay
  publication-title: J Hematol Oncol
– volume: 18
  start-page: 5904
  issue: 22
  year: 2008
  end-page: 5908
  article-title: Targeted intracellular protein degradation induced by a small molecule: en route to chemical proteomics
  publication-title: Bioorg Med Chem Lett
– volume: 146
  start-page: 251
  year: 2018
  end-page: 259
  article-title: Discovery of a Keap1‐dependent peptide PROTAC to knockdown tau by ubiquitination‐proteasome degradation pathway
  publication-title: Eur J Med Chem
– volume: 5
  issue: 11
  year: 2014
  article-title: Cancer cell death induced by novel small molecules degrading the TACC3 protein via the ubiquitin‐proteasome pathway
  publication-title: Cell Death Dis
– year: 2018
– volume: 112
  start-page: 71
  year: 2018
  end-page: 89
  article-title: Hypoxia‐selective allosteric destabilization of activin receptor‐like kinases: a potential therapeutic avenue for prophylaxis of heterotopic ossification
  publication-title: Bone
– volume: 101
  start-page: 80
  year: 2018
  end-page: 93
  article-title: Ubiquitination: friend and foe in cancer
  publication-title: Int J Biochem Cell Biol
– year: 2018
  article-title: Chemical protein degradation approach and its application to epigenetic targets
  publication-title: Chem Rec
– volume: 9
  start-page: 803
  issue: 8
  year: 2018
  end-page: 808
  article-title: New class of selective estrogen receptor degraders (SERDs): expanding the toolbox of PROTAC Degrons
  publication-title: ACS Med Chem Lett
– volume: 31
  start-page: 1951
  issue: 9
  year: 2017
  end-page: 1961
  article-title: Novel BET protein proteolysis‐targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post‐myeloproliferative neoplasm secondary (s) AML cells
  publication-title: Leukemia
– volume: 8
  start-page: 377
  issue: 4
  year: 2018
  end-page: 378
  article-title: Arvinas, Pfizer team up on PROTACs
  publication-title: Cancer Discov
– volume: 7
  start-page: 689
  issue: 7
  year: 2004
  end-page: 697
  article-title: Targeted degradation of proteins by small molecules: a novel tool for functional proteomics
  publication-title: Comb Chem High Throughput Screen
– volume: 73
  start-page: 1064
  issue: 4
  year: 2008
  end-page: 1071
  article-title: Development of an aryl hydrocarbon receptor antagonist using the proteolysis‐targeting chimeric molecules approach: a potential tool for chemoprevention
  publication-title: Mol Pharmacol
– volume: 98
  start-page: 8554
  issue: 15
  year: 2001
  end-page: 8559
  article-title: Protacs: chimeric molecules that target proteins to the Skp1‐Cullin‐F box complex for ubiquitination and degradation
  publication-title: Proc Natl Acad Sci U S a
– volume: 20
  start-page: 518
  issue: 3
  year: 2008
  end-page: 533
  article-title: hSef potentiates EGF‐mediated MAPK signaling through affecting EGFR trafficking and degradation
  publication-title: Cell Signal
– volume: 2
  start-page: 1350
  issue: 12
  year: 2003
  end-page: 1358
  article-title: Development of Protacs to target cancer‐promoting proteins for ubiquitination and degradation
  publication-title: Mol Cell Proteomics
– volume: 8
  start-page: 2058
  issue: 17
  year: 2007
  end-page: 2062
  article-title: Targeted degradation of the aryl hydrocarbon receptor by the PROTAC approach: a useful chemical genetic tool
  publication-title: Chembiochem
– volume: 108
  start-page: 1032
  issue: 5
  year: 2017
  end-page: 1041
  article-title: SNIPER (TACC3) induces cytoplasmic vacuolization and sensitizes cancer cells to Bortezomib
  publication-title: Cancer Sci
– volume: 55
  start-page: 1966
  issue: 6
  year: 2016
  end-page: 1973
  article-title: Small‐molecule PROTACS: new approaches to protein degradation
  publication-title: Angew Chem Int Ed Engl
– volume: 28
  start-page: 256
  issue: 3
  year: 2010
  end-page: 263
  article-title: Harnessing chaperone‐mediated autophagy for the selective degradation of mutant huntingtin protein
  publication-title: Nat Biotechnol
– volume: 14
  start-page: 405
  issue: 4
  year: 2018
  end-page: 412
  article-title: Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands
  publication-title: Nat Chem Biol
– volume: 61
  start-page: 4249
  issue: 9
  year: 2018
  end-page: 4255
  article-title: Chemically induced degradation of anaplastic lymphoma kinase (ALK)
  publication-title: J Med Chem
– volume: 174
  start-page: 138
  year: 2017
  end-page: 144
  article-title: Targeted protein degradation by PROTACs
  publication-title: Pharmacol Ther
– volume: 25
  start-page: 88
  issue: 1
  year: 2018
  end-page: 99
  article-title: A chemoproteomic approach to query the degradable kinome using a multi‐kinase degrader
  publication-title: Cell Chem Biol
– volume: 2
  start-page: 927
  issue: 12
  year: 2016
  end-page: 934
  article-title: Protein degradation by in‐cell self‐assembly of proteolysis targeting chimeras
  publication-title: ACS Cent Sci
– volume: 32
  start-page: 343
  issue: 2
  year: 2018
  end-page: 352
  article-title: BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells
  publication-title: Leukemia
– volume: 132
  start-page: 5820
  issue: 16
  year: 2010
  end-page: 5826
  article-title: Protein knockdown using methyl bestatin‐ligand hybrid molecules: design and synthesis of inducers of ubiquitination‐mediated degradation of cellular retinoic acid‐binding proteins
  publication-title: J Am Chem Soc
– volume: 151
  start-page: 304
  year: 2018
  end-page: 314
  article-title: Proteolysis targeting chimeras (PROTACs) of anaplastic lymphoma kinase (ALK)
  publication-title: Eur J Med Chem
– volume: 173
  start-page: 260
  issue: 1
  year: 2018
  end-page: 274
  article-title: Multiplexed proteome dynamics profiling reveals mechanisms controlling protein homeostasis
  publication-title: Cell
– volume: 91
  start-page: 159
  issue: 3
  year: 2017
  end-page: 166
  article-title: Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules
  publication-title: Mol Pharmacol
– volume: 453
  start-page: 735
  issue: 4
  year: 2014
  end-page: 740
  article-title: Design of a PROTAC that antagonizes and destroys the cancer‐forming X‐protein of the hepatitis B virus
  publication-title: Biochem Biophys Res Commun
– volume: 11
  start-page: 2425
  issue: 7
  year: 1992
  end-page: 2431
  article-title: Targeted degradation of the retinoblastoma protein by human papillomavirus E7‐E6 fusion proteins
  publication-title: EMBO J
– volume: 15
  start-page: 2724
  issue: 11
  year: 2005
  end-page: 2727
  article-title: Use of PROTACS as molecular probes of angiogenesis
  publication-title: Bioorg Med Chem Lett
– volume: 9
  start-page: 1233
  issue: 9
  year: 1999
  end-page: 1238
  article-title: Synthesis and evaluation of geldanamycin‐estradiol hybrids
  publication-title: Bioorg Med Chem Lett
– volume: 126
  start-page: 3748
  issue: 12
  year: 2004
  end-page: 3754
  article-title: Chemical genetic control of protein levels: selective in vivo targeted degradation
  publication-title: J Am Chem Soc
– volume: 61
  start-page: 482
  issue: 2
  year: 2018
  end-page: 491
  article-title: Chemically induced degradation of Sirtuin 2 (Sirt2) by a proteolysis targeting chimera (PROTAC) based on Sirtuin rearranging ligands (SirReals)
  publication-title: J Med Chem
– volume: 32
  start-page: 2224
  issue: 10
  year: 2018
  end-page: 2239
  article-title: Protein targeting chimeric molecules specific for bromodomain and extra‐terminal motif family proteins are active against pre‐clinical models of multiple myeloma
  publication-title: Leukemia
– volume: 57
  start-page: 107
  issue: 1
  year: 2017
  end-page: 123
  article-title: Targeted protein degradation by small molecules
  publication-title: Annu Rev Pharmacol Toxicol
– volume: 27
  start-page: 7201
  issue: 57
  year: 2008
  end-page: 7211
  article-title: Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer
  publication-title: Oncogene
– volume: 28
  start-page: 779
  issue: 7
  year: 2018
  end-page: 781
  article-title: PROTAC‐induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib‐resistant B‐cell malignancies
  publication-title: Cell Res
– volume: 16
  start-page: 136
  issue: 2
  year: 2016
  end-page: 146
  article-title: Protein knockdown technology: application of ubiquitin ligase to cancer therapy
  publication-title: Curr Cancer Drug Targets
– volume: 19
  start-page: 3229
  issue: 10
  year: 2011
  end-page: 3241
  article-title: Development of target protein‐selective degradation inducer for protein knockdown
  publication-title: Bioorg Med Chem
– volume: 26
  start-page: 4865
  issue: 20
  year: 2016
  end-page: 4869
  article-title: Development of BCR‐ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand
  publication-title: Bioorg Med Chem Lett
– volume: 348
  start-page: 1376
  issue: 6241
  year: 2015
  end-page: 1381
  article-title: DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation
  publication-title: Science
– volume: 28
  start-page: 2493
  issue: 14
  year: 2018
  end-page: 2497
  article-title: Development of the first small molecule histone deacetylase 6 (HDAC6) degraders
  publication-title: Bioorg Med Chem Lett
– volume: 61
  start-page: 403
  issue: 2
  year: 2018
  end-page: 404
  article-title: Inducing protein degradation as a therapeutic strategy
  publication-title: J Med Chem
– volume: 55
  start-page: 807
  issue: 2
  year: 2016
  end-page: 810
  article-title: Modular PROTAC design for the degradation of oncogenic BCR‐ABL
  publication-title: Angew Chem Int Ed Engl
– ident: e_1_2_9_49_1
  doi: 10.1126/science.aab1433
– ident: e_1_2_9_41_1
  doi: 10.1016/j.ejmech.2018.01.063
– ident: e_1_2_9_92_1
  doi: 10.1016/j.bioorg.2018.09.005
– ident: e_1_2_9_62_1
  doi: 10.2174/1568009616666151112122502
– ident: e_1_2_9_64_1
  doi: 10.1111/cas.13198
– ident: e_1_2_9_2_1
  doi: 10.1016/j.chembiol.2015.05.009
– ident: e_1_2_9_5_1
  doi: 10.1016/S1097-2765(00)00074-5
– ident: e_1_2_9_99_1
  doi: 10.1021/acs.jmedchem.6b01781
– ident: e_1_2_9_58_1
  doi: 10.1016/j.bmc.2011.03.057
– ident: e_1_2_9_73_1
  doi: 10.1021/acs.jmedchem.6b01816
– ident: e_1_2_9_10_1
  doi: 10.1016/j.chembiol.2017.10.011
– ident: e_1_2_9_94_1
  doi: 10.1038/nrd.2016.211
– ident: e_1_2_9_98_1
  doi: 10.1021/acscentsci.6b00280
– ident: e_1_2_9_14_1
  doi: 10.1007/s10555-017-9698-5
– ident: e_1_2_9_61_1
  doi: 10.1016/j.bmcl.2016.09.041
– ident: e_1_2_9_40_1
  doi: 10.1021/acschembio.7b00985
– ident: e_1_2_9_26_1
  doi: 10.1074/mcp.T300009-MCP200
– ident: e_1_2_9_45_1
  doi: 10.1021/acschembio.5b00442
– ident: e_1_2_9_19_1
  doi: 10.1126/science.aam7340
– ident: e_1_2_9_48_1
  doi: 10.1038/leu.2016.393
– ident: e_1_2_9_38_1
  doi: 10.1038/onc.2008.320
– ident: e_1_2_9_74_1
  doi: 10.1038/s41375-018-0044-x
– ident: e_1_2_9_56_1
  doi: 10.1016/j.febslet.2011.03.019
– ident: e_1_2_9_80_1
  doi: 10.1016/j.ejmech.2018.03.071
– ident: e_1_2_9_35_1
  doi: 10.1038/nn.3637
– ident: e_1_2_9_8_1
  doi: 10.1021/acs.jmedchem.7b01333
– ident: e_1_2_9_88_1
  doi: 10.1021/acs.jmedchem.6b01872
– ident: e_1_2_9_63_1
  doi: 10.1007/978-1-4939-3127-9_42
– volume: 8
  start-page: 377
  issue: 4
  year: 2018
  ident: e_1_2_9_97_1
  article-title: Arvinas, Pfizer team up on PROTACs
  publication-title: Cancer Discov
  doi: 10.1158/2159-8290.CD-NB2018-015
– ident: e_1_2_9_77_1
  doi: 10.1038/s41589-018-0010-y
– ident: e_1_2_9_83_1
  doi: 10.1016/j.ejmech.2018.03.066
– ident: e_1_2_9_6_1
  doi: 10.1016/S0076-6879(05)99054-X
– ident: e_1_2_9_72_1
  doi: 10.1021/acs.jmedchem.8b00506
– ident: e_1_2_9_90_1
  doi: 10.1073/pnas.1803662115
– ident: e_1_2_9_31_1
  doi: 10.1016/j.bmcl.2005.04.008
– ident: e_1_2_9_18_1
  doi: 10.1203/PDR.0b013e3181d35017
– ident: e_1_2_9_42_1
  doi: 10.1016/j.bmcl.2008.07.114
– ident: e_1_2_9_66_1
  doi: 10.1124/mol.116.105569
– ident: e_1_2_9_70_1
  doi: 10.1016/j.bbrc.2018.02.096
– ident: e_1_2_9_27_1
  doi: 10.1016/j.bbrc.2014.10.006
– ident: e_1_2_9_59_1
  doi: 10.1111/cas.12272
– ident: e_1_2_9_11_1
  doi: 10.3390/molecules23081958
– ident: e_1_2_9_71_1
  doi: 10.1038/leu.2017.207
– ident: e_1_2_9_29_1
  doi: 10.2174/1386207043328364
– ident: e_1_2_9_30_1
  doi: 10.1016/j.bmcl.2003.11.042
– ident: e_1_2_9_32_1
  doi: 10.1124/mol.107.040840
– ident: e_1_2_9_96_1
  doi: 10.1016/j.cellsig.2007.11.010
– ident: e_1_2_9_50_1
  doi: 10.1002/anie.201507634
– ident: e_1_2_9_69_1
  doi: 10.1073/pnas.1521738113
– ident: e_1_2_9_21_1
  doi: 10.1021/cb8001792
– ident: e_1_2_9_17_1
  doi: 10.1016/j.cbpa.2016.06.031
– ident: e_1_2_9_23_1
  doi: 10.1016/S0960-894X(00)00208-0
– ident: e_1_2_9_43_1
  doi: 10.1038/nchembio.597
– ident: e_1_2_9_22_1
  doi: 10.1016/S0960-894X(99)00185-7
– ident: e_1_2_9_89_1
  doi: 10.1038/s41422-018-0055-1
– ident: e_1_2_9_54_1
  doi: 10.1021/ja100691p
– ident: e_1_2_9_53_1
  doi: 10.1016/j.cbpa.2017.05.016
– ident: e_1_2_9_57_1
  doi: 10.1002/bies.201700247
– ident: e_1_2_9_28_1
  doi: 10.1021/ja039025z
– ident: e_1_2_9_52_1
  doi: 10.1002/anie.201507978
– ident: e_1_2_9_33_1
  doi: 10.1002/cbic.200700438
– ident: e_1_2_9_51_1
  doi: 10.1039/C7CC03879H
– ident: e_1_2_9_34_1
  doi: 10.1038/nbt.1608
– ident: e_1_2_9_39_1
  doi: 10.1038/aja.2008.26
– ident: e_1_2_9_75_1
  doi: 10.1021/jacs.8b05807
– ident: e_1_2_9_44_1
  doi: 10.1038/nchembio.1858
– ident: e_1_2_9_65_1
  doi: 10.1074/jbc.M116.768853
– ident: e_1_2_9_93_1
  doi: 10.1021/acs.jmedchem.7b00635
– ident: e_1_2_9_67_1
  doi: 10.1021/acsmedchemlett.8b00106
– ident: e_1_2_9_37_1
  doi: 10.1016/j.chembiol.2016.02.016
– ident: e_1_2_9_68_1
  doi: 10.1038/s42003-018-0105-8
– ident: e_1_2_9_46_1
  doi: 10.1021/acschembio.5b00216
– ident: e_1_2_9_4_1
  doi: 10.1016/j.biocel.2018.06.001
– ident: e_1_2_9_81_1
  doi: 10.1021/acs.jmedchem.7b01655
– ident: e_1_2_9_87_1
  doi: 10.1016/j.bmcl.2018.05.057
– ident: e_1_2_9_36_1
  doi: 10.1002/tcr.201800032
– ident: e_1_2_9_12_1
  doi: 10.1016/j.ebiom.2018.09.005
– ident: e_1_2_9_13_1
  doi: 10.1042/EBC20170030
– ident: e_1_2_9_85_1
  doi: 10.1016/j.bcp.2016.07.017
– ident: e_1_2_9_84_1
  doi: 10.1016/j.bone.2018.03.027
– ident: e_1_2_9_86_1
  doi: 10.1038/nchembio.2538
– ident: e_1_2_9_78_1
  doi: 10.1002/psc.2858
– ident: e_1_2_9_76_1
  doi: 10.1016/j.cell.2018.02.030
– ident: e_1_2_9_16_1
  doi: 10.1146/annurev-pharmtox-010715-103507
– ident: e_1_2_9_15_1
  doi: 10.1016/j.chembiol.2017.05.024
– ident: e_1_2_9_9_1
  doi: 10.1016/j.pharmthera.2017.02.027
– ident: e_1_2_9_55_1
  doi: 10.1016/j.bmc.2011.09.041
– ident: e_1_2_9_82_1
  doi: 10.1016/j.bbrc.2018.09.169
– ident: e_1_2_9_91_1
  doi: 10.1016/j.chembiol.2017.10.005
– ident: e_1_2_9_47_1
  doi: 10.1186/s13045-016-0362-2
– ident: e_1_2_9_3_1
  doi: 10.1073/pnas.141230798
– ident: e_1_2_9_24_1
  doi: 10.1002/j.1460-2075.1992.tb05307.x
– ident: e_1_2_9_79_1
  doi: 10.1016/j.bioorg.2018.08.028
– ident: e_1_2_9_95_1
  doi: 10.1016/j.chembiol.2017.09.009
– ident: e_1_2_9_25_1
  doi: 10.1016/S1097-2765(00)80156-2
– ident: e_1_2_9_60_1
  doi: 10.1038/cddis.2014.471
– ident: e_1_2_9_7_1
  doi: 10.1021/acschembio.6b01068
– ident: e_1_2_9_20_1
  doi: 10.1016/S0076-6879(05)99054-X
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Snippet Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This...
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StartPage 21
SubjectTerms Biodegradation
cancer
Drug development
Drug Development - methods
Humans
New technology
PROTAC
Proteasome Endopeptidase Complex - metabolism
protein degradation
Proteins
Proteolysis
Recombinant Fusion Proteins - metabolism
Review
small molecule
Ubiquitin
Ubiquitin-protein ligase
Ubiquitin-Protein Ligases - metabolism
Ubiquitination
Title The PROTAC technology in drug development
URI https://onlinelibrary.wiley.com/doi/abs/10.1002%2Fcbf.3369
https://www.ncbi.nlm.nih.gov/pubmed/30604499
https://www.proquest.com/docview/2167155876
https://www.proquest.com/docview/2163009436
https://pubmed.ncbi.nlm.nih.gov/PMC6590639
Volume 37
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