4k1l

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'''Unreleased structure'''
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{{STRUCTURE_4k1l| PDB=4k1l | SCENE= }}
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===4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 beta-HSD1 inhibitors for the treatment of diabetes===
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{{ABSTRACT_PUBMED_23845218}}
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The entry 4k1l is ON HOLD until Apr 05 2015
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==Disease==
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[[http://www.uniprot.org/uniprot/DHI1_HUMAN DHI1_HUMAN]] Defects in HSD11B1 are a cause of cortisone reductase deficiency (CRD) [MIM:[http://omim.org/entry/604931 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).
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Authors: Loenze, P., Schimanski-Breves, S., Von der Heyden, C., Engel, C.K.
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==Function==
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[[http://www.uniprot.org/uniprot/DHI1_HUMAN 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).
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Description: 4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 beta-HSD1 inhibitors for the treatment of diabetes
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==About this Structure==
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[[4k1l]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4K1L OCA].
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==Reference==
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<ref group="xtra">PMID:023845218</ref><references group="xtra"/><references/>
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[[Category: 11-beta-hydroxysteroid dehydrogenase]]
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[[Category: Engel, C K.]]
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[[Category: Heyden, C Von der.]]
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[[Category: Loenze, P.]]
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[[Category: Schimanski-Breves, S.]]
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[[Category: 11-beta-hsd1]]
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[[Category: 11-beta-hydroxysteroid dehydrogenase 1]]
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[[Category: 11-dh]]
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[[Category: Oxidoreductase-oxidoreductase inhibitor complex]]
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[[Category: Short chain dehydrogenase]]

Revision as of 06:24, 9 April 2014

Template:STRUCTURE 4k1l

Contents

4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 beta-HSD1 inhibitors for the treatment of diabetes

Template:ABSTRACT PUBMED 23845218

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

4k1l is a 4 chain structure. Full crystallographic information is available from OCA.

Reference

  • Bohme T, Engel CK, Farjot G, Gussregen S, Haack T, Tschank G, Ritter K. 1,1-Dioxo-5,6-dihydro-[4,1,2]oxathiazines, a novel class of 11ss-HSD1 inhibitors for the treatment of diabetes. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4685-91. doi:, 10.1016/j.bmcl.2013.05.102. Epub 2013 Jun 11. PMID:23845218 doi:http://dx.doi.org/10.1016/j.bmcl.2013.05.102

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OCA

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