1m51: Difference between revisions
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'''PEPCK complex with a GTP-competitive inhibitor''' | '''PEPCK complex with a GTP-competitive inhibitor''' | ||
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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] | 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] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Dunten, P.]] | [[Category: Dunten, P.]] | ||
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[[Category: Wang, P.]] | [[Category: Wang, P.]] | ||
[[Category: Wertheimer, S J.]] | [[Category: Wertheimer, S J.]] | ||
[[Category: | [[Category: Gluconeogenesis]] | ||
[[Category: | [[Category: Inhibitor]] | ||
[[Category: | [[Category: Xanthine]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:38:28 2008'' | |||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | |||
Revision as of 00:38, 3 May 2008
PEPCK complex with a GTP-competitive inhibitor
OverviewOverview
The analysis of the X-ray structures of two xanthine inhibitors bound to PEPCK and a comparison to the X-ray structure of GTP bound to PEPCK are reported. The SAR at N-1, N-7 and developing SAR at C-8 are consistent with information gained from the X-ray structures of compounds 1 and 2 bound to PEPCK. Representative N-3 modifications of compound 2 that led to the discovery of 3-cyclopropylmethyl and its carboxy analogue as optimal N-3 groups are presented.
DiseaseDisease
Known disease associated with this structure: Hypoglycemia due to PCK1 deficiency (1) OMIM:[261680]
About this StructureAbout this Structure
1M51 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
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 Page seeded by OCA on Sat May 3 00:38:28 2008