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Developmental Effects of Ectopic Expression of the Glucocorticoid Receptor DNA Binding Domain Are Alleviated by an Amino Acid Substitution That Interferes with Homeodomain Binding 
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下载免费PDF全文 Jun Ming Wang Gratien G. Prfontaine Madeleine E. Lemieux Louise Pope Marie-Andre Akimenko Robert J. G. Hach 《Molecular and cellular biology》1999,19(10):7106-7122
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John L. Gilmore James E. Sheppeck Jim Wang T.G. Murali Dhar Cullen Cavallaro Arthur M. Doweyko Lorraine Mckay Mark D. Cunningham Sium F. Habte Steven G. Nadler John H. Dodd John E. Somerville Joel C. Barrish 《Bioorganic & medicinal chemistry letters》2013,23(19):5448-5451
SAR was used to further develop an indazole class of non-steroidal glucocorticoid receptor agonists aided by a GR LBD (ligand-binding domain)-agonist co-crystal structure described in the accompanying paper. Progress towards discovering a dissociated GR agonist guided by human in vitro assays biased the optimization of this compound series towards partial agonists that possessed excellent selectivity against other nuclear hormone receptors. 相似文献