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Page 1
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ 3rd, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK. Taylor AM, et al. Among authors: crawford td. ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. doi: 10.1021/acsmedchemlett.6b00075. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190605 Free PMC article.
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.
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition.
Ghosh S, Taylor A, Chin M, Huang HR, Conery AR, Mertz JA, Salmeron A, Dakle PJ, Mele D, Cote A, Jayaram H, Setser JW, Poy F, Hatzivassiliou G, DeAlmeida-Nagata D, Sandy P, Hatton C, Romero FA, Chiang E, Reimer T, Crawford T, Pardo E, Watson VG, Tsui V, Cochran AG, Zawadzke L, Harmange JC, Audia JE, Bryant BM, Cummings RT, Magnuson SR, Grogan JL, Bellon SF, Albrecht BK, Sims RJ 3rd, Lora JM. Ghosh S, et al. J Biol Chem. 2016 Jun 17;291(25):13014-27. doi: 10.1074/jbc.M115.708560. Epub 2016 Apr 7. J Biol Chem. 2016. PMID: 27056325 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
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Zawadzke L, Albrecht BK, Magnuson SR, Cochran AG, Stokoe D. Crawford TD, et al. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3534-3541. doi: 10.1016/j.bmcl.2017.05.063. Epub 2017 Jun 3. Bioorg Med Chem Lett. 2017. PMID: 28606761
131 results