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Page 1
Discovery of potent dihydro-oxazinoquinolinone inhibitors of GuaB for the treatment of tuberculosis.
Zhou Y, Aliagas I, Wang S, Li CS, Liu Z, Bowman CM, Burdick DJ, Clark KR, Dening TJ, Flygare J, Ganti A, Girgis HS, Hanan EJ, Harris SF, Hu C, Kapadia SB, Koehler MFT, Lai T, Liang J, Liu X, Ma F, Mao J, Nicolai J, Sims J, Unhayaker S, Wai J, Wang X, Wu P, Xu Y, Yen CW, Zhang R, Elfert TF, Tan MW, Kofoed EM, Crawford TD. Zhou Y, et al. Among authors: clark kr. Bioorg Med Chem Lett. 2024 Nov 12:130026. doi: 10.1016/j.bmcl.2024.130026. Online ahead of print. Bioorg Med Chem Lett. 2024. PMID: 39536836
Discovery of GuaB inhibitors with efficacy against Acinetobacter baumannii infection.
Kofoed EM, Aliagas I, Crawford T, Mao J, Harris SF, Xu M, Wang S, Wu P, Ma F, Clark K, Sims J, Xu Y, Peng Y, Skippington E, Yang Y, Reeder J, Ubhayakar S, Baumgardner M, Yan Z, Chen J, Park S, Zhang H, Yen C-W, Lorenzo M, Skelton N, Liang X, Chen L, Hoag B, Li CS, Liu Z, Wai J, Liu X, Liang J, Tan MW. Kofoed EM, et al. mBio. 2024 Oct 16;15(10):e0089724. doi: 10.1128/mbio.00897-24. Epub 2024 Aug 29. mBio. 2024. PMID: 39207111 Free PMC article.
Differential effects of inosine monophosphate dehydrogenase (IMPDH/GuaB) inhibition in Acinetobacter baumannii and Escherichia coli.
Peng Y, Moffat JG, DuPai C, Kofoed EM, Skippington E, Modrusan Z, Gloor SL, Clark K, Xu Y, Li S, Chen L, Liu X, Wu P, Harris SF, Wang S, Crawford TD, Li CS, Liu Z, Wai J, Tan M-W. Peng Y, et al. J Bacteriol. 2024 Oct 24;206(10):e0010224. doi: 10.1128/jb.00102-24. Epub 2024 Sep 5. J Bacteriol. 2024. PMID: 39235234 Free PMC article.
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: clark kr. 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
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.
Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Ramaswamy S, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini M. Bergeron P, et al. ACS Med Chem Lett. 2016 Apr 5;7(6):595-600. doi: 10.1021/acsmedchemlett.6b00044. eCollection 2016 Jun 9. ACS Med Chem Lett. 2016. PMID: 27326333 Free PMC article.
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. 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
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Braun MG, Ashkenazi A, Beveridge RE, Castanedo G, Wallweber HA, Beresini MH, Clark KR, De Bruyn T, Fu L, Gibbons P, Jiang F, Kaufman S, Kan D, Kiefer JR, Leclerc JP, Lemire A, Ly C, Segal E, Sims J, Wang W, Wei W, Zhao L, Schwarz JB, Rudolph J. Braun MG, et al. Among authors: clark kr. J Med Chem. 2024 Jun 13;67(11):8708-8729. doi: 10.1021/acs.jmedchem.3c02425. Epub 2024 May 15. J Med Chem. 2024. PMID: 38748820
Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Gazzard L, Appleton B, Chapman K, Chen H, Clark K, Drobnick J, Goodacre S, Halladay J, Lyssikatos J, Schmidt S, Sideris S, Wiesmann C, Williams K, Wu P, Yen I, Malek S. Gazzard L, et al. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5704-5709. doi: 10.1016/j.bmcl.2014.10.063. Epub 2014 Oct 27. Bioorg Med Chem Lett. 2014. PMID: 25453805
182 results