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Page 1
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM. Shearer BG, et al. Among authors: shearer tw. J Med Chem. 2010 Feb 25;53(4):1857-61. doi: 10.1021/jm900464j. J Med Chem. 2010. PMID: 20128594
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors.
Haffner CD, Becherer JD, Boros EE, Cadilla R, Carpenter T, Cowan D, Deaton DN, Guo Y, Harrington W, Henke BR, Jeune MR, Kaldor I, Milliken N, Petrov KG, Preugschat F, Schulte C, Shearer BG, Shearer T, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Haffner CD, et al. J Med Chem. 2015 Apr 23;58(8):3548-71. doi: 10.1021/jm502009h. Epub 2015 Apr 10. J Med Chem. 2015. PMID: 25828863
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.
Becherer JD, Boros EE, Carpenter TY, Cowan DJ, Deaton DN, Haffner CD, Jeune MR, Kaldor IW, Poole JC, Preugschat F, Rheault TR, Schulte CA, Shearer BG, Shearer TW, Shewchuk LM, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Becherer JD, et al. Among authors: shearer tw. J Med Chem. 2015 Sep 10;58(17):7021-56. doi: 10.1021/acs.jmedchem.5b00992. Epub 2015 Aug 24. J Med Chem. 2015. PMID: 26267483
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.
Evans KA, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ. Evans KA, et al. Among authors: shearer tw. J Med Chem. 2009 Dec 24;52(24):7962-5. doi: 10.1021/jm901434t. J Med Chem. 2009. PMID: 19902954
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model.
Price DJ, Drewry DH, Schaller LT, Thompson BD, Reid PR, Maloney PR, Liang X, Banker P, Buckholz RG, Selley PK, McDonald OB, Smith JL, Shearer TW, Cox RF, Williams SP, Reid RA, Tacconi S, Faggioni F, Piubelli C, Sartori I, Tessari M, Wang TY. Price DJ, et al. Among authors: shearer tw. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1958-1963. doi: 10.1016/j.bmcl.2018.03.034. Epub 2018 Apr 5. Bioorg Med Chem Lett. 2018. PMID: 29653895
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Deng H, O'Keefe H, Davie CP, Lind KE, Acharya RA, Franklin GJ, Larkin J, Matico R, Neeb M, Thompson MM, Lohr T, Gross JW, Centrella PA, O'Donovan GK, Bedard KL, van Vloten K, Mataruse S, Skinner SR, Belyanskaya SL, Carpenter TY, Shearer TW, Clark MA, Cuozzo JW, Arico-Muendel CC, Morgan BA. Deng H, et al. Among authors: shearer tw. J Med Chem. 2012 Aug 23;55(16):7061-79. doi: 10.1021/jm300449x. Epub 2012 Aug 14. J Med Chem. 2012. PMID: 22891645
Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist.
Ignar DM, Goetz AS, Noble KN, Carballo LH, Stroup AE, Fisher JC, Boucheron JA, Brainard TA, Larkin AL, Epperly AH, Shearer TW, Sorensen SD, Speake JD, Hommel JD. Ignar DM, et al. Among authors: shearer tw. J Pharmacol Exp Ther. 2011 Oct;339(1):24-34. doi: 10.1124/jpet.111.180943. Epub 2011 Jun 28. J Pharmacol Exp Ther. 2011. PMID: 21712426
Proteome-wide muscle protein fractional synthesis rates predict muscle mass gain in response to a selective androgen receptor modulator in rats.
Shankaran M, Shearer TW, Stimpson SA, Turner SM, King C, Wong PY, Shen Y, Turnbull PS, Kramer F, Clifton L, Russell A, Hellerstein MK, Evans WJ. Shankaran M, et al. Among authors: shearer tw. Am J Physiol Endocrinol Metab. 2016 Mar 15;310(6):E405-17. doi: 10.1152/ajpendo.00257.2015. Epub 2015 Dec 29. Am J Physiol Endocrinol Metab. 2016. PMID: 26714847 Free article.
20 results