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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: adrian md. J Med Chem. 2014 Feb 13;57(3):849-60. doi: 10.1021/jm401616g. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24446728
Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.
Grese TA, Cho S, Finley DR, Godfrey AG, Jones CD, Lugar CW 3rd, Martin MJ, Matsumoto K, Pennington LD, Winter MA, Adrian MD, Cole HW, Magee DE, Phillips DL, Rowley ER, Short LL, Glasebrook AL, Bryant HU. Grese TA, et al. Among authors: adrian md. J Med Chem. 1997 Jan 17;40(2):146-67. doi: 10.1021/jm9606352. J Med Chem. 1997. PMID: 9003514
A selective estrogen receptor modulator for the treatment of hot flushes.
Wallace OB, Lauwers KS, Dodge JA, May SA, Calvin JR, Hinklin R, Bryant HU, Shetler PK, Adrian MD, Geiser AG, Sato M, Burris TP. Wallace OB, et al. Among authors: adrian md. J Med Chem. 2006 Feb 9;49(3):843-6. doi: 10.1021/jm0509795. J Med Chem. 2006. PMID: 16451049
Benzothiophene and naphthalene derived constrained SERMs.
Wallace OB, Bryant HU, Shetler PK, Adrian MD, Geiser AG. Wallace OB, et al. Among authors: adrian md. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5103-6. doi: 10.1016/j.bmcl.2004.07.072. Bioorg Med Chem Lett. 2004. PMID: 15380208
A new selective estrogen receptor modulator with potent uterine antagonist activity, agonist activity in bone, and minimal ovarian stimulation.
Geiser AG, Hummel CW, Draper MW, Henck JW, Cohen IR, Rudmann DG, Donnelly KB, Adrian MD, Shepherd TA, Wallace OB, McCann DJ, Oldham SW, Bryant HU, Sato M, Dodge JA. Geiser AG, et al. Among authors: adrian md. Endocrinology. 2005 Oct;146(10):4524-35. doi: 10.1210/en.2005-0024. Epub 2005 Jul 7. Endocrinology. 2005. PMID: 16002528
15 results