Glucorticoid receptor

Freedman LP, Luisi BF, Korszum ZR, Basavappa R, Sigler PB, Yamamoto KR (1988) The function and structure of the metal coordination sites within the glucorticoid receptor DNA binding domain. Nature 334 543... 

Glucorticoid receptor (GR) Ligand-induced homodimer Cortisol Palindromic inverted repeat... 

Maule, A.G. and C.B. Schreck. Glucorticoid receptors in leucocytes and gill of juvenile coho salmon (Oncorhynchus kisutch). Gen. Comp. Endocrinol. 77 448-455, 1990. 

Schena, M. and Yamamoto, K.R. (1988) Mammalian glucorticoid receptor derivatives enhance transcription in yeast. Science 241 965-967. 

There exist numerous proven and potential applications for progesterone antagonists (PA) in women s health care. Mifepristone (RU-486), one of the most widely prescribed PAs is of limited clinical use due to lack of selectivity for the progesterone (PR) over the glucorticoid receptor (GR). The resulting undesirable side effect profile has provided the stimulus to search for more selective PAs. These efforts have lead to the discovery of a variety of both steroidal and nonsteroidal entities in recent years. Herein we report the synthesis and SAR of a novel series of pseudosteroids with an improved selectivity of PR over GR. The synthesis of these novel 7-pseudo-steroids 1 has been achieved from trenbolone via an efficient 14-step sequence with overall yields of 10-15%. Various substitutions were incorporated at both the aromatic side chain as well as the D ring. 

Adrenocorticotropic Hormone Receptor Mutations and Isolated Glucorticoid Deficiency... 

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