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Page 1
Structural basis for dual-mode inhibition of the ABC transporter MsbA.
Ho H, Miu A, Alexander MK, Garcia NK, Oh A, Zilberleyb I, Reichelt M, Austin CD, Tam C, Shriver S, Hu H, Labadie SS, Liang J, Wang L, Wang J, Lu Y, Purkey HE, Quinn J, Franke Y, Clark K, Beresini MH, Tan MW, Sellers BD, Maurer T, Koehler MFT, Wecksler AT, Kiefer JR, Verma V, Xu Y, Nishiyama M, Payandeh J, Koth CM. Ho H, et al. Nature. 2018 May;557(7704):196-201. doi: 10.1038/s41586-018-0083-5. Epub 2018 May 2. Nature. 2018. PMID: 29720648
Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA.
Alexander MK, Miu A, Oh A, Reichelt M, Ho H, Chalouni C, Labadie S, Wang L, Liang J, Nickerson NN, Hu H, Yu L, Du M, Yan D, Park S, Kim J, Xu M, Sellers BD, Purkey HE, Skelton NJ, Koehler MFT, Payandeh J, Verma V, Xu Y, Koth CM, Nishiyama M. Alexander MK, et al. Antimicrob Agents Chemother. 2018 Oct 24;62(11):e01142-18. doi: 10.1128/AAC.01142-18. Print 2018 Nov. Antimicrob Agents Chemother. 2018. PMID: 30104274 Free PMC article.
Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors.
Davies CW, Oh AJ, Mroue R, Steffek M, Bruning JM, Xiao Y, Feng S, Jayakar S, Chan E, Arumugam V, Uribe SC, Drummond J, Frommlet A, Lu C, Franke Y, Merchant M, Koeppen H, Quinn JG, Malhotra S, Do S, Gazzard L, Purkey HE, Rudolph J, Mulvihill MM, Koerber JT, Wang W, Evangelista M. Davies CW, et al. Among authors: oh aj. Nat Biotechnol. 2022 May;40(5):769-778. doi: 10.1038/s41587-021-01126-9. Epub 2022 Jan 6. Nat Biotechnol. 2022. PMID: 34992247
Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.
Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, Skelton NJ, Fauber BP, Pan B, Malek S, Stokoe D, Ludlam MJ, Bowman KK, Wu J, Giannetti AM, Starovasnik MA, Mellman I, Jackson PK, Rudolph J, Wang W, Fang G. Maurer T, et al. Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5299-304. doi: 10.1073/pnas.1116510109. Epub 2012 Mar 19. Proc Natl Acad Sci U S A. 2012. PMID: 22431598 Free PMC article.
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, Roberts DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP. Staben ST, et al. J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24432870
Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1.
Kumar S, Waldo JP, Jaipuri FA, Marcinowicz A, Van Allen C, Adams J, Kesharwani T, Zhang X, Metz R, Oh AJ, Harris SF, Mautino MR. Kumar S, et al. Among authors: oh aj. J Med Chem. 2019 Jul 25;62(14):6705-6733. doi: 10.1021/acs.jmedchem.9b00662. Epub 2019 Jul 2. J Med Chem. 2019. PMID: 31264862
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Zeng M, Grandner JM, Bryan MC, Verma V, Larouche-Gauthier R, Leclerc JP, Zhao L, Haghshenas P, Aubert-Nicol S, Yadav A, Ashley M, Chen JZ, Durk M, Samy KE, Nespi M, Levy E, Merrick K, Moffat JG, Murray J, Oh A, Orr C, Segal E, Sims J, Sneeringer C, Prangley M, Vartanian S, Magnuson S, Parr BT. Zeng M, et al. ACS Med Chem Lett. 2023 Aug 24;14(9):1179-1187. doi: 10.1021/acsmedchemlett.3c00142. eCollection 2023 Sep 14. ACS Med Chem Lett. 2023. PMID: 37736184 Free PMC article.
Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Zheng X, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Han B, Ho YC, Kley N, Lin J, Reynolds DJ, Sharma G, Smith CC, Wang Z, Dragovich PS, Oh A, Wang W, Zak M, Wang Y, Yuen PW, Bair KW. Zheng X, et al. Among authors: oh a. Bioorg Med Chem Lett. 2014 Jan 1;24(1):337-43. doi: 10.1016/j.bmcl.2013.11.006. Epub 2013 Nov 14. Bioorg Med Chem Lett. 2014. PMID: 24279990
46 results