2gmv
From Proteopedia
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==Overview== | ==Overview== | ||
| - | New modifications on the C-8 4-aminobenzyl unit of the previously reported | + | New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivative 2 with an IC(50) of 0.29+/-0.08 microM. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new pi-pi interaction. |
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| + | ==Disease== | ||
| + | Known disease associated with this structure: Hypoglycemia due to PCK1 deficiency (1) OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=261680 261680]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: xanthine]] | [[Category: xanthine]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:33:16 2008'' |
Revision as of 15:33, 21 February 2008
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PEPCK complex with a GTP-competitive inhibitor
Contents |
Overview
New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivative 2 with an IC(50) of 0.29+/-0.08 microM. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new pi-pi interaction.
Disease
Known disease associated with this structure: Hypoglycemia due to PCK1 deficiency (1) OMIM:[261680]
About this Structure
2GMV is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Phosphoenolpyruvate carboxykinase (GTP), with EC number 4.1.1.32 Full crystallographic information is available from OCA.
Reference
C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase., Pietranico SL, Foley LH, Huby N, Yun W, Dunten P, Vermeulen J, Wang P, Toth K, Ramsey G, Gubler ML, Wertheimer SJ, Bioorg Med Chem Lett. 2007 Jul 15;17(14):3835-9. Epub 2007 May 22. PMID:17532214
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