3oq1

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Template:STRUCTURE 3oq1

Contents 1 Crystal Structure of 11beta-Hydroxysteroid Dehydrogenase-1 (11b-HSD1) in Complex with Diarylsulfone Inhibitor 2 Disease 3 Function 4 About this Structure 5 See Also 6 Reference

Crystal Structure of 11beta-Hydroxysteroid Dehydrogenase-1 (11b-HSD1) in Complex with Diarylsulfone Inhibitor

Template:ABSTRACT PUBMED 20971000

Disease

[DHI1_HUMAN] Defects in HSD11B1 are a cause of cortisone reductase deficiency (CRD) [MIM:604931]. In CRD, activation of cortisone to cortisol does not occur, resulting in adrenocorticotropin-mediated androgen excess and a phenotype resembling polycystic ovary syndrome (PCOS).

Function

[DHI1_HUMAN] Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the reaction runs only in one direction, from 7-ketocholesterol to 7-beta-hydroxycholesterol (By similarity).

About this Structure

3oq1 is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

• Hydroxysteroid dehydrogenase

Reference

• Yan X, Wang Z, Sudom A, Cardozo M, DeGraffenreid M, Di Y, Fan P, He X, Jaen JC, Labelle M, Liu J, Ma J, McMinn D, Miao S, Sun D, Tang L, Tu H, Ursu S, Walker N, Ye Q, Powers JP. The synthesis and SAR of novel diarylsulfone 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7071-5. Epub 2010 Sep 29. PMID:20971000 doi:10.1016/j.bmcl.2010.09.097