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The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.
Kauppi B, Jakob C, Färnegårdh M, Yang J, Ahola H, Alarcon M, Calles K, Engström O, Harlan J, Muchmore S, Ramqvist AK, Thorell S, Ohman L, Greer J, Gustafsson JA, Carlstedt-Duke J, Carlquist M. Kauppi B, et al. J Biol Chem. 2003 Jun 20;278(25):22748-54. doi: 10.1074/jbc.M212711200. Epub 2003 Apr 9. J Biol Chem. 2003. PMID: 12686538 Free article.
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB. von Geldern TW, et al. Among authors: kauppi b. J Med Chem. 2004 Aug 12;47(17):4213-30. doi: 10.1021/jm0400045. J Med Chem. 2004. PMID: 15293993
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