Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids
Many oncogenic signals originate from abnormal protein-protein interactions that are potential targets for small molecule inhibitors. However, the therapeutic disruption of these interactions has proved elusive. We report here that the naturally-occurring triterpenoid celastrol is an inhibitor of th...
Saved in:
Published in | Oncotarget Vol. 6; no. 32; pp. 32380 - 32395 |
---|---|
Main Authors | , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
United States
Impact Journals LLC
20.10.2015
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
Abstract | Many oncogenic signals originate from abnormal protein-protein interactions that are potential targets for small molecule inhibitors. However, the therapeutic disruption of these interactions has proved elusive. We report here that the naturally-occurring triterpenoid celastrol is an inhibitor of the c-Myc (Myc) oncoprotein, which is over-expressed in many human cancers. Most Myc inhibitors prevent the association between Myc and its obligate heterodimerization partner Max via their respective bHLH-ZIP domains. In contrast, we show that celastrol binds to and alters the quaternary structure of the pre-formed dimer and abrogates its DNA binding. Celastrol contains a reactive quinone methide group that promiscuously forms Michael adducts with numerous target proteins and other free sulfhydryl-containing molecules. Interestingly, triterpenoid derivatives lacking the quinone methide showed enhanced specificity and potency against Myc. As with other Myc inhibitors, these analogs rapidly reduced the abundance of Myc protein and provoked a global energy crisis marked by ATP depletion, neutral lipid accumulation, AMP-activated protein kinase activation, cell cycle arrest and apoptosis. They also inhibited the proliferation of numerous established human cancer cell lines as well as primary myeloma explants that were otherwise resistant to JQ1, a potent indirect Myc inhibitor. N-Myc amplified neuroblastoma cells showed similar responses and, in additional, underwent neuronal differentiation. These studies indicate that certain pharmacologically undesirable properties of celastrol such as Michael adduct formation can be eliminated while increasing selectivity and potency toward Myc and N-Myc. This, together with their low in vivo toxicity, provides a strong rationale for pursuing the development of additional Myc-specific triterpenoid derivatives. |
---|---|
AbstractList | Many oncogenic signals originate from abnormal protein-protein interactions that are potential targets for small molecule inhibitors. However, the therapeutic disruption of these interactions has proved elusive. We report here that the naturally-occurring triterpenoid celastrol is an inhibitor of the c-Myc (Myc) oncoprotein, which is over-expressed in many human cancers. Most Myc inhibitors prevent the association between Myc and its obligate heterodimerization partner Max via their respective bHLH-ZIP domains. In contrast, we show that celastrol binds to and alters the quaternary structure of the pre-formed dimer and abrogates its DNA binding. Celastrol contains a reactive quinone methide group that promiscuously forms Michael adducts with numerous target proteins and other free sulfhydryl-containing molecules. Interestingly, triterpenoid derivatives lacking the quinone methide showed enhanced specificity and potency against Myc. As with other Myc inhibitors, these analogs rapidly reduced the abundance of Myc protein and provoked a global energy crisis marked by ATP depletion, neutral lipid accumulation, AMP-activated protein kinase activation, cell cycle arrest and apoptosis. They also inhibited the proliferation of numerous established human cancer cell lines as well as primary myeloma explants that were otherwise resistant to JQ1, a potent indirect Myc inhibitor. N-Myc amplified neuroblastoma cells showed similar responses and, in additional, underwent neuronal differentiation. These studies indicate that certain pharmacologically undesirable properties of celastrol such as Michael adduct formation can be eliminated while increasing selectivity and potency toward Myc and N-Myc. This, together with their low in vivo toxicity, provides a strong rationale for pursuing the development of additional Myc-specific triterpenoid derivatives. Many oncogenic signals originate from abnormal protein-protein interactions that are potential targets for small molecule inhibitors. However, the therapeutic disruption of these interactions has proved elusive. We report here that the naturally-occurring triterpenoid celastrol is an inhibitor of the c-Myc (Myc) oncoprotein, which is over-expressed in many human cancers. Most Myc inhibitors prevent the association between Myc and its obligate heterodimerization partner Max via their respective bHLH-ZIP domains. In contrast, we show that celastrol binds to and alters the quaternary structure of the pre-formed dimer and abrogates its DNA binding. Celastrol contains a reactive quinone methide group that promiscuously forms Michael adducts with numerous target proteins and other free sulfhydryl-containing molecules. Interestingly, triterpenoid derivatives lacking the quinone methide showed enhanced specificity and potency against Myc. As with other Myc inhibitors, these analogs rapidly reduced the abundance of Myc protein and provoked a global energy crisis marked by ATP depletion, neutral lipid accumulation, AMP-activated protein kinase activation, cell cycle arrest and apoptosis. They also inhibited the proliferation of numerous established human cancer cell lines as well as primary myeloma explants that were otherwise resistant to JQ1, a potent indirect Myc inhibitor. N-Myc amplified neuroblastoma cells showed similar responses and, in additional, underwent neuronal differentiation. These studies indicate that certain pharmacologically undesirable properties of celastrol such as Michael adduct formation can be eliminated while increasing selectivity and potency toward Myc and N-Myc. This, together with their low in vivo toxicity, provides a strong rationale for pursuing the development of additional Myc-specific triterpenoid derivatives. |
Author | Pendelton, Kelsey Lazo, John S Holien, Toril Cosford, Nicholas D P Wang, Huabo Hu, Angela Arsenian-Henriksson, Marie Misund, Kristine Oliynyk, Ganna Prochownik, Edward V Sundan, Anders Raveendra-Panickar, Dhanya Teriete, Peter Eiseman, Julie |
AuthorAffiliation | 8 The Department of Microbiology and Molecular Genetics, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA 7 Department of Microbiology and Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden 1 Section of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA 4 The Department of Chemical Biology and Pharmacology, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA 5 The University of Pittsburgh Cancer Institute, Pittsburgh, PA, USA 6 Department of Cancer Research and Molecular Medicine and The K. G. Jebsen Center for Myeloma Research, Norwegian University of Science and Technology, Trondheim, Norway 3 The Department of Pharmacology, The University of Virginia School of Medicine, Charlottesville, Virginia, USA 2 Cell Death and Survival Networks Research Program, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA |
AuthorAffiliation_xml | – name: 5 The University of Pittsburgh Cancer Institute, Pittsburgh, PA, USA – name: 6 Department of Cancer Research and Molecular Medicine and The K. G. Jebsen Center for Myeloma Research, Norwegian University of Science and Technology, Trondheim, Norway – name: 8 The Department of Microbiology and Molecular Genetics, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – name: 3 The Department of Pharmacology, The University of Virginia School of Medicine, Charlottesville, Virginia, USA – name: 4 The Department of Chemical Biology and Pharmacology, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – name: 1 Section of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – name: 2 Cell Death and Survival Networks Research Program, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA – name: 7 Department of Microbiology and Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden |
Author_xml | – sequence: 1 givenname: Huabo surname: Wang fullname: Wang, Huabo organization: Section of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – sequence: 2 givenname: Peter surname: Teriete fullname: Teriete, Peter organization: Cell Death and Survival Networks Research Program, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA – sequence: 3 givenname: Angela surname: Hu fullname: Hu, Angela organization: Section of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – sequence: 4 givenname: Dhanya surname: Raveendra-Panickar fullname: Raveendra-Panickar, Dhanya organization: Cell Death and Survival Networks Research Program, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA – sequence: 5 givenname: Kelsey surname: Pendelton fullname: Pendelton, Kelsey organization: Section of Hematology/Oncology, Children's Hospital of Pittsburgh of UPMC, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA – sequence: 6 givenname: John S surname: Lazo fullname: Lazo, John S organization: The Department of Pharmacology, The University of Virginia School of Medicine, Charlottesville, Virginia, USA – sequence: 7 givenname: Julie surname: Eiseman fullname: Eiseman, Julie organization: The University of Pittsburgh Cancer Institute, Pittsburgh, PA, USA – sequence: 8 givenname: Toril surname: Holien fullname: Holien, Toril organization: Department of Cancer Research and Molecular Medicine and The K. G. Jebsen Center for Myeloma Research, Norwegian University of Science and Technology, Trondheim, Norway – sequence: 9 givenname: Kristine surname: Misund fullname: Misund, Kristine organization: Department of Cancer Research and Molecular Medicine and The K. G. Jebsen Center for Myeloma Research, Norwegian University of Science and Technology, Trondheim, Norway – sequence: 10 givenname: Ganna surname: Oliynyk fullname: Oliynyk, Ganna organization: Department of Microbiology and Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden – sequence: 11 givenname: Marie surname: Arsenian-Henriksson fullname: Arsenian-Henriksson, Marie organization: Department of Microbiology and Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden – sequence: 12 givenname: Nicholas D P surname: Cosford fullname: Cosford, Nicholas D P organization: Cell Death and Survival Networks Research Program, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA – sequence: 13 givenname: Anders surname: Sundan fullname: Sundan, Anders organization: Department of Cancer Research and Molecular Medicine and The K. G. Jebsen Center for Myeloma Research, Norwegian University of Science and Technology, Trondheim, Norway – sequence: 14 givenname: Edward V surname: Prochownik fullname: Prochownik, Edward V organization: The Department of Microbiology and Molecular Genetics, The University of Pittsburgh Medical Center, Pittsburgh, PA, USA |
BackLink | https://www.ncbi.nlm.nih.gov/pubmed/26474287$$D View this record in MEDLINE/PubMed http://kipublications.ki.se/Default.aspx?queryparsed=id:132313271$$DView record from Swedish Publication Index |
BookMark | eNpVkdtOAyEQhompsbX23iuzL7AVFtjDjYmpx6TGG700hAW2RbewATz07aW29kAyYRjm_4bwn4KesUYBcI7gGJU5zi6tETZwN1NhnCOUH4EBqkiVZpTi3l7eByPv32FclBRlVp2AfpaTgmRlMQBvN9opERJt5rrWQVuT2CYR6dMyBv9J5iooZ6VeKOeTepkI1XIfnG0TbuTulGrju0iSSXA6KjplrJb-DBw3vPVqtNmH4PXu9mXykE6f7x8n19NUEJKHlEJcUrJ6q6xLTjPcZJWCpEQkh3WdUwkLwivUqLKI1YLEvlLkEnMlBaVC4CGo1lz_rbrPmnVOL7hbMst1zK1km_qHXgXziiGc4RgFitqrtTY2LCJQmeB4e4g4uDF6zmb2i8UvRAWEEQDXAOGs9041Wy2C7M8ptnOKrZyKkov9mVvBvy_4F5CClvI |
CitedBy_id | crossref_primary_10_1016_j_ejmech_2017_07_013 crossref_primary_10_1016_j_prp_2022_153851 crossref_primary_10_1093_jxb_erw440 crossref_primary_10_3390_cells11243974 crossref_primary_10_1186_s13765_020_00565_3 crossref_primary_10_1021_acs_jmedchem_0c00894 crossref_primary_10_3390_cancers13071668 crossref_primary_10_1016_j_chembiol_2015_12_005 crossref_primary_10_1002_gcc_22388 crossref_primary_10_1155_2022_1948657 crossref_primary_10_1007_s40259_019_00370_5 crossref_primary_10_3389_fendo_2018_00129 crossref_primary_10_1016_j_heliyon_2024_e28411 crossref_primary_10_3390_cancers13112678 crossref_primary_10_1101_gr_222935_117 crossref_primary_10_3892_ijmm_2018_3519 crossref_primary_10_1016_j_ejmech_2024_116194 crossref_primary_10_1158_0008_5472_CAN_20_2959 crossref_primary_10_1016_j_heliyon_2022_e11407 crossref_primary_10_3390_molecules25214950 crossref_primary_10_3390_ijms222312883 crossref_primary_10_1016_j_celrep_2023_112830 crossref_primary_10_1038_s41375_018_0036_x crossref_primary_10_1007_s11240_017_1257_9 crossref_primary_10_1016_j_chembiol_2019_02_009 crossref_primary_10_3390_ijms20010120 crossref_primary_10_1038_s41392_023_01589_z crossref_primary_10_1080_13543784_2019_1605354 crossref_primary_10_1186_s12943_020_01291_6 crossref_primary_10_3389_fcell_2023_1244321 crossref_primary_10_3389_fcell_2017_00010 crossref_primary_10_1038_s41598_018_28107_4 crossref_primary_10_3390_ijms22073458 crossref_primary_10_1074_jbc_TM118_003336 crossref_primary_10_1016_j_jmb_2018_04_008 crossref_primary_10_18632_oncotarget_16325 crossref_primary_10_3390_genes8040107 crossref_primary_10_3390_ijms25116099 crossref_primary_10_3389_fphar_2018_00104 |
Cites_doi | 10.1073/pnas.90.3.960 10.1038/nature07260 10.1124/mol.109.054858 10.1126/science.2251503 10.1038/sj.onc.1206641 10.1177/1087057113478168 10.1007/s12185-013-1291-2 10.1038/322848a0 10.1158/1078-0432.CCR-13-0275 10.1111/j.1476-5381.2011.01449.x 10.1021/cr400713r 10.18632/oncotarget.4327 10.1091/mbc.e07-10-1004 10.1007/s00280-008-0774-y 10.1038/nrc2231 10.1016/j.cell.2012.03.003 10.1371/journal.pone.0026634 10.1124/jpet.110.170555 10.1158/1940-6207.CAPR-11-0420 10.1371/journal.pone.0037699 10.1021/ja208359a 10.1128/MCB.8.2.963 10.1016/j.cell.2011.08.017 10.1038/nrm3311 10.1158/1535-7163.MCT-14-0774-T 10.1016/j.chembiol.2015.04.019 10.3390/molecules190710177 10.1021/jm501440q 10.1128/MCB.01535-08 10.1038/nature10334 10.1073/pnas.1108190108 10.1021/ja900616b 10.1016/j.stem.2009.07.003 10.1371/journal.pone.0041070 10.1016/j.bbagrm.2014.03.005 10.1038/sj.onc.1202746 10.1182/blood-2011-08-371567 10.1021/jm801278g 10.1016/j.bmcl.2012.10.013 10.1038/nature09504 10.1146/annurev.ge.20.120186.002045 10.18632/oncotarget.1108 10.1073/pnas.76.6.2779 10.1016/S0092-8674(02)01284-9 10.1016/j.exphem.2006.06.019 10.1101/gad.205542.112 10.1158/1535-7163.MCT-07-0005 10.1016/j.canlet.2008.01.043 10.1016/j.chembiol.2008.09.011 10.1083/jcb.201112044 10.1016/j.bbrc.2010.03.050 10.1038/nature06526 10.1016/j.canlet.2010.10.025 10.1016/j.semcancer.2014.04.012 10.1016/j.cbpa.2010.06.169 10.1371/journal.pone.0105381 10.2174/0929867321666140414111333 10.2174/156802611794072632 10.1074/jbc.M114.580662 10.1073/pnas.75.5.2458 10.1158/0008-5472.CAN-05-4529 10.1038/306494a0 10.1016/j.cbpa.2008.07.023 10.1016/j.chembiol.2014.09.001 10.1371/journal.pone.0097285 10.1177/1947601910377494 10.1006/jmbi.2001.4537 10.3109/10428194.2014.924116 10.1016/j.canlet.2009.09.006 10.1016/j.bcp.2006.08.014 10.1007/s00109-010-0669-3 10.1002/anie.200900929 10.1111/joim.12237 10.1073/pnas.1222404110 10.1101/gad.17420111 10.1007/978-1-4614-0659-4_3 10.1074/jbc.272.28.17416 10.1182/blood-2006-10-050807 10.1097/00043426-200404000-00003 10.1002/cmdc.201402189 |
ContentType | Journal Article |
Copyright | Copyright: © 2015 Wang et al. 2015 |
Copyright_xml | – notice: Copyright: © 2015 Wang et al. 2015 |
DBID | CGR CUY CVF ECM EIF NPM AAYXX CITATION 5PM ADTPV AOWAS D8T ZZAVC |
DOI | 10.18632/oncotarget.6116 |
DatabaseName | Medline MEDLINE MEDLINE (Ovid) MEDLINE MEDLINE PubMed CrossRef PubMed Central (Full Participant titles) SwePub SwePub Articles SWEPUB Freely available online SwePub Articles full text |
DatabaseTitle | MEDLINE Medline Complete MEDLINE with Full Text PubMed MEDLINE (Ovid) CrossRef |
DatabaseTitleList | MEDLINE |
Database_xml | – sequence: 1 dbid: NPM name: PubMed url: https://proxy.k.utb.cz/login?url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=PubMed sourceTypes: Index Database – sequence: 2 dbid: EIF name: MEDLINE url: https://proxy.k.utb.cz/login?url=https://www.webofscience.com/wos/medline/basic-search sourceTypes: Index Database |
DeliveryMethod | fulltext_linktorsrc |
EISSN | 1949-2553 |
EndPage | 32395 |
ExternalDocumentID | oai_prod_swepub_kib_ki_se_132313271 10_18632_oncotarget_6116 26474287 |
Genre | Research Support, Non-U.S. Gov't Journal Article Research Support, N.I.H., Extramural |
GrantInformation_xml | – fundername: NCI NIH HHS grantid: R01 CA174713 – fundername: NCI NIH HHS grantid: P30CA047904 – fundername: NCI NIH HHS grantid: P30 CA047904 – fundername: NCI NIH HHS grantid: R01CA140624 – fundername: NCI NIH HHS grantid: R01 CA140624 |
GroupedDBID | --- 53G ADBBV ADRAZ AENEX ALMA_UNASSIGNED_HOLDINGS AOIJS BAWUL CGR CUY CVF DIK ECM EIF FRJ GX1 HYE KQ8 M48 M~E NPM OK1 PGMZT RPM AAYXX CITATION 5PM ADTPV AOWAS D8T ZZAVC |
ID | FETCH-LOGICAL-c446t-5038542553db8a523f29e0481460bb65d074a91fe870487453d8c6d3aedc55cc3 |
IEDL.DBID | RPM |
ISSN | 1949-2553 |
IngestDate | Sun Oct 27 03:39:15 EDT 2024 Tue Sep 17 21:14:51 EDT 2024 Fri Aug 23 03:07:26 EDT 2024 Sat Sep 28 08:27:25 EDT 2024 |
IsDoiOpenAccess | true |
IsOpenAccess | true |
IsPeerReviewed | false |
IsScholarly | true |
Issue | 32 |
Keywords | quinone methide neuroblastoma 10074-G5 myeloma 10058-F4 BET inhibitors |
Language | English |
License | This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
LinkModel | DirectLink |
MergedId | FETCHMERGED-LOGICAL-c446t-5038542553db8a523f29e0481460bb65d074a91fe870487453d8c6d3aedc55cc3 |
OpenAccessLink | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741700/ |
PMID | 26474287 |
PageCount | 16 |
ParticipantIDs | swepub_primary_oai_prod_swepub_kib_ki_se_132313271 pubmedcentral_primary_oai_pubmedcentral_nih_gov_4741700 crossref_primary_10_18632_oncotarget_6116 pubmed_primary_26474287 |
PublicationCentury | 2000 |
PublicationDate | 2015-10-20 |
PublicationDateYYYYMMDD | 2015-10-20 |
PublicationDate_xml | – month: 10 year: 2015 text: 2015-10-20 day: 20 |
PublicationDecade | 2010 |
PublicationPlace | United States |
PublicationPlace_xml | – name: United States |
PublicationTitle | Oncotarget |
PublicationTitleAlternate | Oncotarget |
PublicationYear | 2015 |
Publisher | Impact Journals LLC |
Publisher_xml | – name: Impact Journals LLC |
References | Felsher (23) 2014; 4 Prochownik (55) 1997; 272 Kukowska (69) 1986; 322 Bergsagel (81) 2011; 146 Malkin (84) 2004; 26 Ronai (41) 2007; 13 McClendon (1) 2007; 450 Pan (43) 2010; 290 Bister (57) 2001; 307 Bahar (58) 2009; 52 Metallo (34) 2009; 131 Prochownik (12) 2015; 1849 Dou (40) 2006; 66 Schwalbe (79) 2009; 48 Henriksson (26) 2013; 110 Hardie (63) 2011; 25 Lallemand-Breitenbach (5) 2012; 198 Mustata (13) 2011; 11 Metallo (14) 2010; 14 Sethi (51) 2011; 164 Henriksson (39) 2014; 9 Cole (70) 1986; 20 Zhou (42) 2008; 264 Hawley (64) 2012; 13 Fletcher (32) 2013; 23 Felsher (24) 2014; 276 VanAntwerp (54) 1993; 90 Sims (82) 2011; 108 Chinnaiyan (6) 2014; 20 Kesari (11) 2014; 21 Brown (83) 2011; 478 Cuchillo (35) 2012; 7 Prochownik (59) 2015; 2 Qazilbash (75) 2015; 56 Penn (18) 2008; 8 Lin (66) 2014; 9 Kriwacki (15) 2012; 725 Sethi (52) 2011; 303 Prochownik (28) 2003; 22 Liu (65) 2006; 34 Bross (53) 2011; 6 Croce (73) 1983; 306 Vogt (9) 2010; 1 Morano (50) 2008; 19 Vogt (36) 2009; 76 Lee (49) 2006; 72 Silverman (48) 2011; 133 Dang (19) 2012; 149 Huggins (4) 2015; 22 Nienhuis (71) 1988; 8 Lu (47) 2014; 19 Henderson (7) 2014; 27 Kaarniranta (44) 2010; 394 Berg (3) 2011; 348 Prochownik (17) 1999; 18 Damsky (68) 1979; 76 Sundan (76) 2012; 120 Prochownik (62) 2014; 289 Fletcher (31) 2015; 58 Gallo (67) 1978; 75 Burley (60) 2003; 112 Kizaki (78) 2011; 39 Joerger (16) 2014; 114 Fletcher (85) 2014; 9 Evan (25) 2013; 27 Evan (22) 2008; 455 Aggarwal (45) 2010; 88 Wells (10) 2014; 21 Berg (2) 2008; 12 Sethi (46) 2012; 5 Bellosta (61) 2009; 29 Prochownik (29) 2007; 6 Tomasson (27) 2015; 14 Sundan (86) 2013; 18 Weintraub (56) 1990; 250 Dalton (72) 2009; 5 Aggarwal (77) 2007; 109 West (80) 2010; 468 Metallo (33) 2008; 15 Eiseman (37) 2009; 63 Prochownik (20) 2012; 7 Bergsagel (74) 2013; 97 Prochownik (30) 2013; 4 Prochownik (21) 2015; 6 Carroll (8) 2015; 1855 Eiseman (38) 2010; 335 |
References_xml | – volume: 90 start-page: 960 issue: 3 year: 1993 ident: 54 article-title: Differential patterns of DNA binding by myc and max proteins publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.90.3.960 contributor: fullname: VanAntwerp – volume: 455 start-page: 679 issue: 7213 year: 2008 ident: 22 article-title: Modelling Myc inhibition as a cancer therapy publication-title: Nature doi: 10.1038/nature07260 contributor: fullname: Evan – volume: 76 start-page: 491 issue: 3 year: 2009 ident: 36 article-title: Stabilizers of the Max homodimer identified in virtual ligand screening inhibit Myc function publication-title: Mol Pharmacol doi: 10.1124/mol.109.054858 contributor: fullname: Vogt – volume: 250 start-page: 1149 issue: 4984 year: 1990 ident: 56 article-title: Sequence-specific DNA binding by the c-Myc protein publication-title: Science doi: 10.1126/science.2251503 contributor: fullname: Weintraub – volume: 22 start-page: 6151 issue: 40 year: 2003 ident: 28 article-title: Low molecular weight inhibitors of Myc-Max interaction and function publication-title: Oncogene doi: 10.1038/sj.onc.1206641 contributor: fullname: Prochownik – volume: 18 start-page: 637 issue: 6 year: 2013 ident: 86 article-title: A method for measurement of drug sensitivity of myeloma cells co-cultured with bone marrow stromal cells publication-title: J Biomol Screen doi: 10.1177/1087057113478168 contributor: fullname: Sundan – volume: 97 start-page: 313 issue: 3 year: 2013 ident: 74 article-title: Molecular pathogenesis of multiple myeloma: basic and clinical updates publication-title: Int J Hematol doi: 10.1007/s12185-013-1291-2 contributor: fullname: Bergsagel – volume: 39 start-page: 1117 issue: 5 year: 2011 ident: 78 article-title: Quinone methide tripterine, celastrol, induces apoptosis in human myeloma cells via NF-kappaB pathway publication-title: Int J Oncol contributor: fullname: Kizaki – volume: 322 start-page: 848 issue: 6082 year: 1986 ident: 69 article-title: Deregulated expression of c-myc by murine erythroleukaemia cells prevents differentiation publication-title: Nature doi: 10.1038/322848a0 contributor: fullname: Kukowska – volume: 20 start-page: 4442 issue: 17 year: 2014 ident: 6 article-title: Molecular pathways: targeting ETS gene fusions in cancer publication-title: Clin Cancer Res doi: 10.1158/1078-0432.CCR-13-0275 contributor: fullname: Chinnaiyan – volume: 164 start-page: 1506 issue: 5 year: 2011 ident: 51 article-title: Celastrol inhibits proliferation and induces chemosensitization through down-regulation of NF-kappaB and STAT3 regulated gene products in multiple myeloma cells publication-title: Br J Pharmacol doi: 10.1111/j.1476-5381.2011.01449.x contributor: fullname: Sethi – volume: 114 start-page: 6844 issue: 13 year: 2014 ident: 16 article-title: Pathological unfoldomics of uncontrolled chaos: intrinsically disordered proteins and human diseases publication-title: Chem Rev doi: 10.1021/cr400713r contributor: fullname: Joerger – volume: 6 start-page: 15857 issue: 18 year: 2015 ident: 21 article-title: Structurally diverse c-Myc inhibitors share a common mechanism of action involving ATP depletion publication-title: Oncotarget doi: 10.18632/oncotarget.4327 contributor: fullname: Prochownik – volume: 19 start-page: 1104 issue: 3 year: 2008 ident: 50 article-title: Activation of heat shock and antioxidant responses by the natural product celastrol: transcriptional signatures of a thiol-targeted molecule publication-title: Mol Biol Cell doi: 10.1091/mbc.e07-10-1004 contributor: fullname: Morano – volume: 63 start-page: 615 issue: 4 year: 2009 ident: 37 article-title: Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice publication-title: Cancer Chemother Pharmacol doi: 10.1007/s00280-008-0774-y contributor: fullname: Eiseman – volume: 8 start-page: 976 issue: 12 year: 2008 ident: 18 article-title: Reflecting on 25 years with MYC publication-title: Nat Rev Cancer doi: 10.1038/nrc2231 contributor: fullname: Penn – volume: 149 start-page: 22 issue: 1 year: 2012 ident: 19 article-title: MYC on the path to cancer publication-title: Cell doi: 10.1016/j.cell.2012.03.003 contributor: fullname: Dang – volume: 6 start-page: e26634 issue: 10 year: 2011 ident: 53 article-title: Quantitative proteomics reveals cellular targets of celastrol publication-title: PLoS One doi: 10.1371/journal.pone.0026634 contributor: fullname: Bross – volume: 335 start-page: 715 issue: 3 year: 2010 ident: 38 article-title: In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization publication-title: J Pharmacol Exp Ther doi: 10.1124/jpet.110.170555 contributor: fullname: Eiseman – volume: 5 start-page: 631 issue: 4 year: 2012 ident: 46 article-title: Celastrol suppresses growth and induces apoptosis of human hepatocellular carcinoma through the modulation of STAT3/JAK2 signaling cascade in vitro and in vivo publication-title: Cancer Prev Res (Phila) doi: 10.1158/1940-6207.CAPR-11-0420 contributor: fullname: Sethi – volume: 7 start-page: e37699 issue: 5 year: 2012 ident: 20 article-title: Mitochondrial structure, function and dynamics are temporally controlled by c-Myc publication-title: PLoS One doi: 10.1371/journal.pone.0037699 contributor: fullname: Prochownik – volume: 13 start-page: 6769 issue: 22 Pt 1 year: 2007 ident: 41 article-title: Preclinical studies of celastrol and acetyl isogambogic acid in melanoma publication-title: Clin Cancer Res contributor: fullname: Ronai – volume: 133 start-page: 19634 issue: 49 year: 2011 ident: 48 article-title: Remarkable stereospecific conjugate additions to the Hsp90 inhibitor celastrol publication-title: J Am Chem Soc doi: 10.1021/ja208359a contributor: fullname: Silverman – volume: 8 start-page: 963 issue: 2 year: 1988 ident: 71 article-title: An oligomer complementary to c-myc mRNA inhibits proliferation of HL-60 promyelocytic cells and induces differentiation publication-title: Mol Cell Biol doi: 10.1128/MCB.8.2.963 contributor: fullname: Nienhuis – volume: 146 start-page: 904 issue: 6 year: 2011 ident: 81 article-title: BET bromodomain inhibition as a therapeutic strategy to target c-Myc publication-title: Cell doi: 10.1016/j.cell.2011.08.017 contributor: fullname: Bergsagel – volume: 13 start-page: 251 issue: 4 year: 2012 ident: 64 article-title: AMPK: a nutrient and energy sensor that maintains energy homeostasis publication-title: Nat Rev Mol Cell Biol doi: 10.1038/nrm3311 contributor: fullname: Hawley – volume: 1855 start-page: 183 issue: 2 year: 2015 ident: 8 article-title: Transcription factors and chromatin proteins as therapeutic targets in cancer publication-title: Biochim Biophys Acta contributor: fullname: Carroll – volume: 14 start-page: 1286 issue: 6 year: 2015 ident: 27 article-title: Small Molecule MYC Inhibitor Conjugated to Integrin-Targeted Nanoparticles Extends Survival in a Mouse Model of Disseminated Multiple Myeloma publication-title: Mol Cancer Ther doi: 10.1158/1535-7163.MCT-14-0774-T contributor: fullname: Tomasson – volume: 2 start-page: pii issue: 2 year: 2015 ident: 59 article-title: A quantitative, surface plasmon resonance-based approach to evaluating DNA binding by the c-Myc oncoprotein and its disruption by small molecule inhibitors publication-title: J Biol Methods contributor: fullname: Prochownik – volume: 22 start-page: 689 issue: 6 year: 2015 ident: 4 article-title: Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions publication-title: Chem Biol doi: 10.1016/j.chembiol.2015.04.019 contributor: fullname: Huggins – volume: 4 issue: 6 year: 2014 ident: 23 article-title: MYC activation is a hallmark of cancer initiation and maintenance publication-title: Cold Spring Harb Perspect Med contributor: fullname: Felsher – volume: 19 start-page: 10177 issue: 7 year: 2014 ident: 47 article-title: Design, synthesis and biological evaluation of C6-modified celastrol derivatives as potential antitumor agents publication-title: Molecules doi: 10.3390/molecules190710177 contributor: fullname: Lu – volume: 58 start-page: 3002 issue: 7 year: 2015 ident: 31 article-title: Perturbation of the c-Myc-Max protein-protein interaction via synthetic alpha-helix mimetics publication-title: J Med Chem doi: 10.1021/jm501440q contributor: fullname: Fletcher – volume: 29 start-page: 3424 issue: 12 year: 2009 ident: 61 article-title: Identification of domains responsible for ubiquitin-dependent degradation of dMyc by glycogen synthase kinase 3beta and casein kinase 1 kinases publication-title: Mol Cell Biol doi: 10.1128/MCB.01535-08 contributor: fullname: Bellosta – volume: 478 start-page: 524 issue: 7370 year: 2011 ident: 83 article-title: RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia publication-title: Nature doi: 10.1038/nature10334 contributor: fullname: Brown – volume: 108 start-page: 16669 issue: 40 year: 2011 ident: 82 article-title: Targeting MYC dependence in cancer by inhibiting BET bromodomains publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.1108190108 contributor: fullname: Sims – volume: 131 start-page: 7390 issue: 21 year: 2009 ident: 34 article-title: Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc publication-title: J Am Chem Soc doi: 10.1021/ja900616b contributor: fullname: Metallo – volume: 5 start-page: 141 issue: 2 year: 2009 ident: 72 article-title: The cell cycle and Myc intersect with mechanisms that regulate pluripotency and reprogramming publication-title: Cell Stem Cell doi: 10.1016/j.stem.2009.07.003 contributor: fullname: Dalton – volume: 7 start-page: e41070 issue: 7 year: 2012 ident: 35 article-title: The impact of small molecule binding on the energy landscape of the intrinsically disordered protein C-myc publication-title: PLoS One doi: 10.1371/journal.pone.0041070 contributor: fullname: Cuchillo – volume: 1849 start-page: 525 issue: 5 year: 2015 ident: 12 article-title: Small-molecule inhibitors of the Myc oncoprotein publication-title: Biochim Biophys Acta doi: 10.1016/j.bbagrm.2014.03.005 contributor: fullname: Prochownik – volume: 18 start-page: 3004 issue: 19 year: 1999 ident: 17 article-title: MYC oncogenes and human neoplastic disease publication-title: Oncogene doi: 10.1038/sj.onc.1202746 contributor: fullname: Prochownik – volume: 120 start-page: 2450 issue: 12 year: 2012 ident: 76 article-title: Addiction to c-MYC in multiple myeloma publication-title: Blood doi: 10.1182/blood-2011-08-371567 contributor: fullname: Sundan – volume: 52 start-page: 1247 issue: 5 year: 2009 ident: 58 article-title: Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model publication-title: J Med Chem doi: 10.1021/jm801278g contributor: fullname: Bahar – volume: 23 start-page: 370 issue: 1 year: 2013 ident: 32 article-title: Pharmacophore identification of c-Myc inhibitor 10074-G5 publication-title: Bioorg Med Chem Lett doi: 10.1016/j.bmcl.2012.10.013 contributor: fullname: Fletcher – volume: 468 start-page: 1067 issue: 7327 year: 2010 ident: 80 article-title: Selective inhibition of BET bromodomains publication-title: Nature doi: 10.1038/nature09504 contributor: fullname: West – volume: 20 start-page: 361 year: 1986 ident: 70 article-title: The myc oncogene: its role in transformation and differentiation publication-title: Annu Rev Genet doi: 10.1146/annurev.ge.20.120186.002045 contributor: fullname: Cole – volume: 4 start-page: 936 issue: 6 year: 2013 ident: 30 article-title: Disruption of Myc-Max heterodimerization with improved cell-penetrating analogs of the small molecule 10074-G5 publication-title: Oncotarget doi: 10.18632/oncotarget.1108 contributor: fullname: Prochownik – volume: 76 start-page: 2779 issue: 6 year: 1979 ident: 68 article-title: Human promyelocytic leukemia cells in culture differentiate into macrophage-like cells when treated with a phorbol diester publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.76.6.2779 contributor: fullname: Damsky – volume: 112 start-page: 193 issue: 2 year: 2003 ident: 60 article-title: X-ray structures of Myc-Max and Mad-Max recognizing DNA. Molecular bases of regulation by proto-oncogenic transcription factors publication-title: Cell doi: 10.1016/S0092-8674(02)01284-9 contributor: fullname: Burley – volume: 34 start-page: 1480 issue: 11 year: 2006 ident: 65 article-title: A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia publication-title: Exp Hematol doi: 10.1016/j.exphem.2006.06.019 contributor: fullname: Liu – volume: 27 start-page: 504 issue: 5 year: 2013 ident: 25 article-title: Inhibition of Myc family proteins eradicates KRas-driven lung cancer in mice publication-title: Genes Dev doi: 10.1101/gad.205542.112 contributor: fullname: Evan – volume: 6 start-page: 2399 issue: 9 year: 2007 ident: 29 article-title: Improved low molecular weight Myc-Max inhibitors publication-title: Mol Cancer Ther doi: 10.1158/1535-7163.MCT-07-0005 contributor: fullname: Prochownik – volume: 264 start-page: 101 issue: 1 year: 2008 ident: 42 article-title: Celastrol inhibits the growth of human glioma xenografts in nude mice through suppressing VEGFR expression publication-title: Cancer Lett doi: 10.1016/j.canlet.2008.01.043 contributor: fullname: Zhou – volume: 15 start-page: 1149 issue: 11 year: 2008 ident: 33 article-title: Structural rationale for the coupled binding and unfolding of the c-Myc oncoprotein by small molecules publication-title: Chem Biol doi: 10.1016/j.chembiol.2008.09.011 contributor: fullname: Metallo – volume: 198 start-page: 11 issue: 1 year: 2012 ident: 5 article-title: The cell biology of disease: Acute promyelocytic leukemia, arsenic, and PML bodies publication-title: J Cell Biol doi: 10.1083/jcb.201112044 contributor: fullname: Lallemand-Breitenbach – volume: 394 start-page: 439 issue: 3 year: 2010 ident: 44 article-title: Celastrol: Molecular targets of Thunder God Vine publication-title: Biochem Biophys Res Commun doi: 10.1016/j.bbrc.2010.03.050 contributor: fullname: Kaarniranta – volume: 450 start-page: 1001 issue: 7172 year: 2007 ident: 1 article-title: Reaching for high-hanging fruit in drug discovery at protein-protein interfaces publication-title: Nature doi: 10.1038/nature06526 contributor: fullname: McClendon – volume: 303 start-page: 9 issue: 1 year: 2011 ident: 52 article-title: Molecular targets of celastrol derived from Thunder of God Vine: potential role in the treatment of inflammatory disorders and cancer publication-title: Cancer Lett doi: 10.1016/j.canlet.2010.10.025 contributor: fullname: Sethi – volume: 27 start-page: 20 year: 2014 ident: 7 article-title: Targeting the beta-catenin nuclear transport pathway in cancer publication-title: Semin Cancer Biol doi: 10.1016/j.semcancer.2014.04.012 contributor: fullname: Henderson – volume: 14 start-page: 481 issue: 4 year: 2010 ident: 14 article-title: Intrinsically disordered proteins are potential drug targets publication-title: Curr Opin Chem Biol doi: 10.1016/j.cbpa.2010.06.169 contributor: fullname: Metallo – volume: 9 start-page: e105381 issue: 8 year: 2014 ident: 66 article-title: Inhibition of c-Myc overcomes cytotoxic drug resistance in acute myeloid leukemia cells by promoting differentiation publication-title: PLoS One doi: 10.1371/journal.pone.0105381 contributor: fullname: Lin – volume: 21 start-page: 3227 issue: 28 year: 2014 ident: 11 article-title: bHLH Transcription factors inhibitors for cancer therapy: general features for in silico drug design publication-title: Curr Med Chem doi: 10.2174/0929867321666140414111333 contributor: fullname: Kesari – volume: 11 start-page: 248 issue: 3 year: 2011 ident: 13 article-title: Discovery of modulators of protein-protein interactions: current approaches and limitations publication-title: Curr Top Med Chem doi: 10.2174/156802611794072632 contributor: fullname: Mustata – volume: 289 start-page: 25382 issue: 36 year: 2014 ident: 62 article-title: c-Myc programs fatty acid metabolism and dictates acetyl-CoA abundance and fate publication-title: J Biol Chem doi: 10.1074/jbc.M114.580662 contributor: fullname: Prochownik – volume: 75 start-page: 2458 issue: 5 year: 1978 ident: 67 article-title: Terminal differentiation of human promyelocytic leukemia cells induced by dimethyl sulfoxide and other polar compounds publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.75.5.2458 contributor: fullname: Gallo – volume: 66 start-page: 4758 issue: 9 year: 2006 ident: 40 article-title: Celastrol, a triterpene extracted from the Chinese “Thunder of God Vine,” is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice publication-title: Cancer Res doi: 10.1158/0008-5472.CAN-05-4529 contributor: fullname: Dou – volume: 306 start-page: 494 issue: 5942 year: 1983 ident: 73 article-title: Association of amplified oncogene c-myc with an abnormally banded chromosome 8 in a human leukaemia cell line publication-title: Nature doi: 10.1038/306494a0 contributor: fullname: Croce – volume: 348 start-page: 139 year: 2011 ident: 3 article-title: Small-molecule modulators of c-Myc/Max and Max/Max interactions publication-title: Curr Top Microbiol Immunol contributor: fullname: Berg – volume: 12 start-page: 464 issue: 4 year: 2008 ident: 2 article-title: Inhibition of transcription factors with small organic molecules publication-title: Curr Opin Chem Biol doi: 10.1016/j.cbpa.2008.07.023 contributor: fullname: Berg – volume: 21 start-page: 1102 issue: 9 year: 2014 ident: 10 article-title: Small-molecule inhibitors of protein-protein interactions: progressing toward the reality publication-title: Chem Biol doi: 10.1016/j.chembiol.2014.09.001 contributor: fullname: Wells – volume: 9 start-page: e97285 issue: 5 year: 2014 ident: 39 article-title: Targeting of the MYCN protein with small molecule c-MYC inhibitors publication-title: PLoS One doi: 10.1371/journal.pone.0097285 contributor: fullname: Henriksson – volume: 1 start-page: 650 issue: 6 year: 2010 ident: 9 article-title: Therapeutic Targeting of Myc publication-title: Genes Cancer doi: 10.1177/1947601910377494 contributor: fullname: Vogt – volume: 307 start-page: 1395 issue: 5 year: 2001 ident: 57 article-title: Structure, function, and dynamics of the dimerization and DNA-binding domain of oncogenic transcription factor v-Myc publication-title: J Mol Biol doi: 10.1006/jmbi.2001.4537 contributor: fullname: Bister – volume: 56 start-page: 602 issue: 3 year: 2015 ident: 75 article-title: Chromosome 8q24. 1/c-MYC abnormality: a marker for high-risk myeloma publication-title: Leuk Lymphoma doi: 10.3109/10428194.2014.924116 contributor: fullname: Qazilbash – volume: 290 start-page: 182 issue: 2 year: 2010 ident: 43 article-title: Celastrol, a novel HSP90 inhibitor, depletes Bcr-Abl and induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation publication-title: Cancer Lett doi: 10.1016/j.canlet.2009.09.006 contributor: fullname: Pan – volume: 72 start-page: 1311 issue: 10 year: 2006 ident: 49 article-title: Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid publication-title: Biochem Pharmacol doi: 10.1016/j.bcp.2006.08.014 contributor: fullname: Lee – volume: 88 start-page: 1243 issue: 12 year: 2010 ident: 45 article-title: Celastrol suppresses invasion of colon and pancreatic cancer cells through the downregulation of expression of CXCR4 chemokine receptor publication-title: J Mol Med (Berl) doi: 10.1007/s00109-010-0669-3 contributor: fullname: Aggarwal – volume: 48 start-page: 5853 issue: 32 year: 2009 ident: 79 article-title: Molecular mechanism of inhibition of the human protein complex Hsp90-Cdc37, a kinome chaperone-cochaperone, by triterpene celastrol publication-title: Angew Chem Int Ed Engl doi: 10.1002/anie.200900929 contributor: fullname: Schwalbe – volume: 276 start-page: 52 issue: 1 year: 2014 ident: 24 article-title: Inactivation of MYC reverses tumorigenesis publication-title: J Intern Med doi: 10.1111/joim.12237 contributor: fullname: Felsher – volume: 110 start-page: 10258 issue: 25 year: 2013 ident: 26 article-title: MYC inhibition induces metabolic changes leading to accumulation of lipid droplets in tumor cells publication-title: Proc Natl Acad Sci U S A doi: 10.1073/pnas.1222404110 contributor: fullname: Henriksson – volume: 25 start-page: 1895 issue: 18 year: 2011 ident: 63 article-title: AMP-activated protein kinase: an energy sensor that regulates all aspects of cell function publication-title: Genes Dev doi: 10.1101/gad.17420111 contributor: fullname: Hardie – volume: 725 start-page: 27 year: 2012 ident: 15 article-title: Intrinsic protein flexibility in regulation of cell proliferation: advantages for signaling and opportunities for novel therapeutics publication-title: Adv Exp Med Biol doi: 10.1007/978-1-4614-0659-4_3 contributor: fullname: Kriwacki – volume: 272 start-page: 17416 issue: 28 year: 1997 ident: 55 article-title: Distinct roles for MAX protein isoforms in proliferation and apoptosis publication-title: J Biol Chem doi: 10.1074/jbc.272.28.17416 contributor: fullname: Prochownik – volume: 109 start-page: 2727 issue: 7 year: 2007 ident: 77 article-title: Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation publication-title: Blood doi: 10.1182/blood-2006-10-050807 contributor: fullname: Aggarwal – volume: 26 start-page: 227 issue: 4 year: 2004 ident: 84 article-title: Factors influencing survival in children with recurrent neuroblastoma publication-title: J Pediatr Hematol Oncol doi: 10.1097/00043426-200404000-00003 contributor: fullname: Malkin – volume: 9 start-page: 2274 issue: 10 year: 2014 ident: 85 article-title: Discovery of methyl 4′-methyl-5-(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)-[1,1′;-biphenyl]-3-carboxylate, an improved small-molecule inhibitor of c-Myc-max dimerization publication-title: ChemMedChem doi: 10.1002/cmdc.201402189 contributor: fullname: Fletcher |
SSID | ssj0000547829 |
Score | 2.3539314 |
Snippet | Many oncogenic signals originate from abnormal protein-protein interactions that are potential targets for small molecule inhibitors. However, the therapeutic... |
SourceID | swepub pubmedcentral crossref pubmed |
SourceType | Open Access Repository Aggregation Database Index Database |
StartPage | 32380 |
SubjectTerms | Antineoplastic Agents, Phytogenic - metabolism Antineoplastic Agents, Phytogenic - pharmacology Apoptosis - drug effects Basic Helix-Loop-Helix Leucine Zipper Transcription Factors - antagonists & inhibitors Basic Helix-Loop-Helix Leucine Zipper Transcription Factors - metabolism Cell Cycle Checkpoints - drug effects Cell Line, Tumor Cell Proliferation - drug effects Dose-Response Relationship, Drug Drug Design Humans Medicin och hälsovetenskap Molecular Targeted Therapy Neoplasms - drug therapy Neoplasms - genetics Neoplasms - metabolism Neoplasms - pathology Priority Research Paper Protein Binding Protein Multimerization Protein Structure, Quaternary Proto-Oncogene Proteins c-myc - antagonists & inhibitors Proto-Oncogene Proteins c-myc - genetics Proto-Oncogene Proteins c-myc - metabolism Signal Transduction - drug effects Structure-Activity Relationship Time Factors Transfection Triterpenes - metabolism Triterpenes - pharmacology Tumor Cells, Cultured |
SummonAdditionalLinks | – databaseName: Scholars Portal Open Access Journals dbid: M48 link: http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwnV1LT4NAEN5ovXgxGl_4yh68eNhaYHeBgzHG2DQm9WSTXgzZFynRgLY1af-9M0DbYDx54ADsQviGYeZjZ78l5Do2vtbAfJhQUcB45nOmstixnrQhdwkKhOBE4eGLHIz481iMN9OjGwBnf1I7XE9qNP3oLr6W9-Dwd-jwsQyD2xJ1DKrC6a70fblNdgKU5cJCvibZr5W-OYTDpBmr_KsjKgNLHiGLaIWpdWz6XTfZUhetIlJ_n-w1qSR9qG1_QLZccUje6m8YzYtJrqtyLFpm1LDhEja1oBMsfyltjr-rqV5S4yB9xmJ1qgq72WN5gUPwzlIU63dTwKTM7eyIjPpPr48D1iyhwAzwvDlDsRcBbilCq2MFpDMLEocSMVz2tJbCQgahEj9z4LYcle9DGxswk4KHFMKY8Jh0irJwp4RGUaacC4RSGi4NdjTAxVRstfMtT7jwyM0KsfSzVspIkWEg0OkG6BSB9shJjeS65Qp3j0QtjNcNUAa7fabIJ5UcNnREkUGPBLU12l0A0rQ5_p7jls5cChQcJSsj_-zftzsnu5A7VSquQe-CdObTb3cJ-clcX1Wv3Q-d_-xl priority: 102 providerName: Scholars Portal |
Title | Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids |
URI | https://www.ncbi.nlm.nih.gov/pubmed/26474287 https://pubmed.ncbi.nlm.nih.gov/PMC4741700 http://kipublications.ki.se/Default.aspx?queryparsed=id:132313271 |
Volume | 6 |
hasFullText | 1 |
inHoldings | 1 |
isFullTextHit | |
isPrint | |
link | http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwnV1LT-MwEB7RnvaCQLBQXvKBCwe3edh5HBGiIKQiDovUyyryK2q0i1OVrrT8e2aStBCOHBIpifP6xs7MxJ8_A1xmJtQaMx8uVRpxUYaCqzJzPEhsLFxOAiE0UHj2mNw_i4e5nO-A3IyFaUj7Rldj__dl7KtFw61cvpjJhic2eZrdCHSDaRBMBjDACvopRW8FvQV6vbzrksySOJrUpHPQEKvHSRjSrEUYBqSULPS80dYFfaVH9kREG8cz3YPdLmJk1-2T7cOO8wfwu_1UscovKt2wrlhdMsNnb7io_2xBLJfaVvRXmuk3ZhxGycRJZ8rbjy1eeeppd5aRJr9bLZ2vK_t6CM_T218397ybKYEbTOfWnDRdJLY-GVudKcwtyyh3pAQjkkDrRFoMFFQelg5bpyCB-9hmBq2h8CWlNCb-CUNfe3cMLE1L5VwkldJ4aTSXwZRLZVa70IpcyBFcbRArlq0gRkGJBAFdfABdENAjOGqR3Jbc4D6CtIfxtgCpXfePYCVoVK87o48gaq3RPwUhLbr9fypaildXYKZNypRpePLt253CDwyRGrHWKDiD4Xr1z51jGLLWFzC4m4e4nonsoqmC7_T35QA |
link.rule.ids | 230,315,730,783,787,888,2228,24332,27938,27939,53806,53808 |
linkProvider | National Library of Medicine |
linkToHtml | http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwnV1JT9wwFH6i9NBeuqjbdAEfuPTgTBY7y7FCRcMyiANUXKrIWzQRxRnBIAG_vu9lGQi39pBDEmfzZ-e9L_n8GWAnN5HWyHy4VFnMRRUJrqrc8TC1iXAFGYTQQOH5cTo7Ewfn8nwD5DAWphXtG10H_s9l4OtFq61cXprpoBObnsx3BYbBLAynz-A59tcwfUTSO0tvgXGv6H9K5mkSTxtyOmil1UEaRTRvESYCGdGFUTxaB6GnAsmRjWgbevZew6_hpjvFyUVws9KBuX_i5_jPT_UGXvXJKPvR7X4LG86_g9_dW5DVflHrVtDFmooZPr_DRd2yBQloGlvTB2-m75hxmICT3J0pbx_WeO3pJ76zjOz-3dXS-aa21-_hbO_n6e6M95MwcINMccXJLkZix5aJ1blC2lrFhSOTGZGGWqfSYg6iiqhy2PEFeecnNjcItMLak9KY5ANs-sa7T8CyrFLOxVIpjafGlmCQzancahdZUQg5ge8DFOWy89ooiaMQguUDgiUhOIGPHUTrkgOgE8hG4K0LkJH2eA8i0Rpq9zU_gbiDeXwIVmnZb7-oaSmvXYkknkwvs-jzf19uG17MTudH5dH-8eEXeImZWOsJG4dfYXN1deO-Ybaz0ltt2_4LPssFMw |
linkToPdf | http://utb.summon.serialssolutions.com/2.0.0/link/0/eLvHCXMwnV3LTtwwFL1qqYS6aYtK22lp8aIbFs7TzmNZQUf0MYgFSKhSFfkVTURxRjBIwNf33iQzEJYsskjivHzs3Hvik2OAr4WJtUbmw6XKEy7qWHBVF45HmU2FK8kghH4Unh1lh6fi55k8ezDVVyfaN7oJ_L-LwDfzTlu5uDDhSicWHs_2BYbBPIrCha3D5_AC-2xUPCDqva23wNhXDgOTRZYmYUtuB528OsjimOYuwmQgJ8owiknrQPRYJDmyEu3Cz_Q1_FndeK86OQ-ulzowd488HZ_0ZG_g1ZCUsm99kS145vxb-Nu_DVnj543uhF2srZnhs1tc1A2bk5CmtQ19-Gb6lhmHiTjJ3pny9n6NN54G851lZPvvLhfOt4292obT6feT_UM-TMbADTLGJSfbGIkdXKZWFwrpa52UjsxmRBZpnUmLuYgq49rhC0CQh35qC4OAK6xBKY1J38GGb737ACzPa-VcIpXSeGpsEQZZnSqsdrEVpZAT2FvBUS16z42KuAqhWN2jWBGKE3jfw7QuuQJ1AvkIwHUBMtQe70E0OmPtofYnkPRQjw_BKq2G7ecNLdWVq5DMk_llHn988uV2YfP4YFr9_nH06xO8xISss4ZNoh3YWF5eu8-Y9Cz1l655_wdIqAez |
openUrl | ctx_ver=Z39.88-2004&ctx_enc=info%3Aofi%2Fenc%3AUTF-8&rfr_id=info%3Asid%2Fsummon.serialssolutions.com&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.atitle=Direct+inhibition+of+c-Myc-Max+heterodimers+by+celastrol+and+celastrol-inspired+triterpenoids&rft.jtitle=Oncotarget&rft.au=Wang%2C+Huabo&rft.au=Teriete%2C+Peter&rft.au=Hu%2C+Angela&rft.au=Raveendra-Panickar%2C+Dhanya&rft.date=2015-10-20&rft.pub=Impact+Journals+LLC&rft.eissn=1949-2553&rft.volume=6&rft.issue=32&rft.spage=32380&rft.epage=32395&rft_id=info:doi/10.18632%2Foncotarget.6116&rft_id=info%3Apmid%2F26474287&rft.externalDBID=PMC4741700 |
thumbnail_l | http://covers-cdn.summon.serialssolutions.com/index.aspx?isbn=/lc.gif&issn=1949-2553&client=summon |
thumbnail_m | http://covers-cdn.summon.serialssolutions.com/index.aspx?isbn=/mc.gif&issn=1949-2553&client=summon |
thumbnail_s | http://covers-cdn.summon.serialssolutions.com/index.aspx?isbn=/sc.gif&issn=1949-2553&client=summon |