4k1l: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
{{STRUCTURE_4k1l| PDB=4k1l | SCENE= }} | |||
===4,4-Dioxo-5,6-dihydro-[1,4,3]oxathiazines, a novel class of 11 beta-HSD1 inhibitors for the treatment of diabetes=== | |||
{{ABSTRACT_PUBMED_23845218}} | |||
==Disease== | |||
[[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). | |||
==Function== | |||
[[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). | |||
==About this Structure== | |||
[[4k1l]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4K1L OCA]. | |||
==Reference== | |||
<ref group="xtra">PMID:023845218</ref><references group="xtra"/><references/> | |||
[[Category: 11-beta-hydroxysteroid dehydrogenase]] | |||
[[Category: Engel, C K.]] | |||
[[Category: Heyden, C Von der.]] | |||
[[Category: Loenze, P.]] | |||
[[Category: Schimanski-Breves, S.]] | |||
[[Category: 11-beta-hsd1]] | |||
[[Category: 11-beta-hydroxysteroid dehydrogenase 1]] | |||
[[Category: 11-dh]] | |||
[[Category: Oxidoreductase-oxidoreductase inhibitor complex]] | |||
[[Category: Short chain dehydrogenase]] | |||
Revision as of 06:24, 9 April 2014
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:https://dx.doi.org/10.1016/j.bmcl.2013.05.102
