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Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
Durham TB, Toth JL, Klimkowski VJ, Cao JX, Siesky AM, Alexander-Chacko J, Wu GY, Dixon JT, McGee JE, Wang Y, Guo SY, Cavitt RN, Schindler J, Thibodeaux SJ, Calvert NA, Coghlan MJ, Sindelar DK, Christe M, Kiselyov VV, Michael MD, Sloop KW. Durham TB, et al. Among authors: coghlan mj. J Biol Chem. 2015 Aug 14;290(33):20044-59. doi: 10.1074/jbc.M115.638205. Epub 2015 Jun 17. J Biol Chem. 2015. PMID: 26085101 Free PMC article.
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Carson MW, Luz JG, Suen C, Montrose C, Zink R, Ruan X, Cheng C, Cole H, Adrian MD, Kohlman DT, Mabry T, Snyder N, Condon B, Maletic M, Clawson D, Pustilnik A, Coghlan MJ. Carson MW, et al. Among authors: coghlan mj. J Med Chem. 2014 Feb 13;57(3):849-60. doi: 10.1021/jm401616g. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24446728
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC. Kym PR, et al. Among authors: coghlan mj. J Med Chem. 2003 Mar 13;46(6):1016-30. doi: 10.1021/jm020335m. J Med Chem. 2003. PMID: 12620078
trans-Activation and repression properties of the novel nonsteroid glucocorticoid receptor ligand 2,5-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5-(1-methylcyclohexen-3-y1)-1H-[1]benzopyrano[3,4-f]quinoline (A276575) and its four stereoisomers.
Lin CW, Nakane M, Stashko M, Falls D, Kuk J, Miller L, Huang R, Tyree C, Miner JN, Rosen J, Kym PR, Coghlan MJ, Carter G, Lane BC. Lin CW, et al. Among authors: coghlan mj. Mol Pharmacol. 2002 Aug;62(2):297-303. doi: 10.1124/mol.62.2.297. Mol Pharmacol. 2002. PMID: 12130681
40 results