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Page 1
Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.
Crawford TD, Ndubaku CO, Chen H, Boggs JW, Bravo BJ, Delatorre K, Giannetti AM, Gould SE, Harris SF, Magnuson SR, McNamara E, Murray LJ, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Stanley M, Vitorino P, Wang L, West K, Wu P, Ye W. Crawford TD, et al. J Med Chem. 2014 Apr 24;57(8):3484-93. doi: 10.1021/jm500155b. Epub 2014 Apr 9. J Med Chem. 2014. PMID: 24673130
Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.
Wang L, Stanley M, Boggs JW, Crawford TD, Bravo BJ, Giannetti AM, Harris SF, Magnuson SR, Nonomiya J, Schmidt S, Wu P, Ye W, Gould SE, Murray LJ, Ndubaku CO, Chen H. Wang L, et al. Among authors: crawford td. Bioorg Med Chem Lett. 2014 Sep 15;24(18):4546-4552. doi: 10.1016/j.bmcl.2014.07.071. Epub 2014 Aug 2. Bioorg Med Chem Lett. 2014. PMID: 25139565
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.
Ndubaku CO, Crawford TD, Chen H, Boggs JW, Drobnick J, Harris SF, Jesudason R, McNamara E, Nonomiya J, Sambrone A, Schmidt S, Smyczek T, Vitorino P, Wang L, Wu P, Yeung S, Chen J, Chen K, Ding CZ, Wang T, Xu Z, Gould SE, Murray LJ, Ye W. Ndubaku CO, et al. Among authors: crawford td. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. doi: 10.1021/acsmedchemlett.5b00174. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288693 Free PMC article.
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Crawford TD, Tsui V, Flynn EM, Wang S, Taylor AM, Côté A, Audia JE, Beresini MH, Burdick DJ, Cummings R, Dakin LA, Duplessis M, Good AC, Hewitt MC, Huang HR, Jayaram H, Kiefer JR, Jiang Y, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Crawford TD, et al. J Med Chem. 2016 Jun 9;59(11):5391-402. doi: 10.1021/acs.jmedchem.6b00264. Epub 2016 May 31. J Med Chem. 2016. PMID: 27219867
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S. Crawford TD, et al. J Med Chem. 2016 Dec 8;59(23):10549-10563. doi: 10.1021/acs.jmedchem.6b01022. Epub 2016 Sep 28. J Med Chem. 2016. PMID: 27682507
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S. Romero FA, et al. Among authors: crawford td. J Med Chem. 2017 Nov 22;60(22):9162-9183. doi: 10.1021/acs.jmedchem.7b00796. Epub 2017 Sep 21. J Med Chem. 2017. PMID: 28892380
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Bronner SM, Murray J, Romero FA, Lai KW, Tsui V, Cyr P, Beresini MH, de Leon Boenig G, Chen Z, Choo EF, Clark KR, Crawford TD, Jayaram H, Kaufman S, Li R, Li Y, Liao J, Liang X, Liu W, Ly J, Maher J, Wai J, Wang F, Zheng A, Zhu X, Magnuson S. Bronner SM, et al. Among authors: crawford td. J Med Chem. 2017 Dec 28;60(24):10151-10171. doi: 10.1021/acs.jmedchem.7b01372. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29155580
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Wang S, et al. Among authors: crawford td. J Med Chem. 2018 Oct 25;61(20):9301-9315. doi: 10.1021/acs.jmedchem.8b01225. Epub 2018 Oct 5. J Med Chem. 2018. PMID: 30289257
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.
Di Lello P, Pastor R, Murray JM, Blake RA, Cohen F, Crawford TD, Drobnick J, Drummond J, Kategaya L, Kleinheinz T, Maurer T, Rougé L, Zhao X, Wertz I, Ndubaku C, Tsui V. Di Lello P, et al. Among authors: crawford td. J Med Chem. 2017 Dec 28;60(24):10056-10070. doi: 10.1021/acs.jmedchem.7b01293. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29166018
127 results