2gmv

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[[Image:2gmv.gif|left|200px]]
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{{STRUCTURE_2gmv| PDB=2gmv | SCENE= }}
{{STRUCTURE_2gmv| PDB=2gmv | SCENE= }}
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'''PEPCK complex with a GTP-competitive inhibitor'''
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===PEPCK complex with a GTP-competitive inhibitor===
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==Overview==
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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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The line below this paragraph, {{ABSTRACT_PUBMED_17532214}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17532214 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17532214}}
==Disease==
==Disease==
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==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/17532214 17532214]
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:[http://www.ncbi.nlm.nih.gov/pubmed/17532214 17532214]
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X-ray structures of two xanthine inhibitors bound to PEPCK and N-3 modifications of substituted 1,8-dibenzylxanthines., Foley LH, Wang P, Dunten P, Ramsey G, Gubler ML, Wertheimer SJ, Bioorg Med Chem Lett. 2003 Nov 3;13(21):3871-4. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/14552798 14552798]
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Crystal structure of human cytosolic phosphoenolpyruvate carboxykinase reveals a new GTP-binding site., Dunten P, Belunis C, Crowther R, Hollfelder K, Kammlott U, Levin W, Michel H, Ramsey GB, Swain A, Weber D, Wertheimer SJ, J Mol Biol. 2002 Feb 15;316(2):257-64. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11851336 11851336]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Inhibitor]]
[[Category: Inhibitor]]
[[Category: Xanthine]]
[[Category: Xanthine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:17:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:11:36 2008''

Revision as of 12:11, 27 July 2008

Image:2gmv.png

Template:STRUCTURE 2gmv

Contents

PEPCK complex with a GTP-competitive inhibitor

Template:ABSTRACT PUBMED 17532214

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. 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

X-ray structures of two xanthine inhibitors bound to PEPCK and N-3 modifications of substituted 1,8-dibenzylxanthines., Foley LH, Wang P, Dunten P, Ramsey G, Gubler ML, Wertheimer SJ, Bioorg Med Chem Lett. 2003 Nov 3;13(21):3871-4. PMID:14552798

Crystal structure of human cytosolic phosphoenolpyruvate carboxykinase reveals a new GTP-binding site., Dunten P, Belunis C, Crowther R, Hollfelder K, Kammlott U, Levin W, Michel H, Ramsey GB, Swain A, Weber D, Wertheimer SJ, J Mol Biol. 2002 Feb 15;316(2):257-64. PMID:11851336

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