1nhx
From Proteopedia
(New page: 200px<br /> <applet load="1nhx" size="450" color="white" frame="true" align="right" spinBox="true" caption="1nhx, resolution 2.10Å" /> '''PEPCK COMPLEX WITH ...) |
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caption="1nhx, resolution 2.10Å" /> | caption="1nhx, resolution 2.10Å" /> | ||
'''PEPCK COMPLEX WITH A GTP-COMPETITIVE INHIBITOR'''<br /> | '''PEPCK COMPLEX WITH A GTP-COMPETITIVE INHIBITOR'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1NHX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MN, NA, PEP, FTB and EDO as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phosphoenolpyruvate_carboxykinase_(GTP) Phosphoenolpyruvate carboxykinase (GTP)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.1.1.32 4.1.1.32] Full crystallographic information is available from [http:// | + | 1NHX is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MN:'>MN</scene>, <scene name='pdbligand=NA:'>NA</scene>, <scene name='pdbligand=PEP:'>PEP</scene>, <scene name='pdbligand=FTB:'>FTB</scene> and <scene name='pdbligand=EDO:'>EDO</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Phosphoenolpyruvate_carboxykinase_(GTP) Phosphoenolpyruvate carboxykinase (GTP)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.1.1.32 4.1.1.32] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NHX OCA]. |
==Reference== | ==Reference== | ||
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[[Category: xanthine]] | [[Category: xanthine]] | ||
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Revision as of 14:29, 15 February 2008
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PEPCK COMPLEX WITH A GTP-COMPETITIVE INHIBITOR
Contents |
Overview
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.
Disease
Known disease associated with this structure: Hypoglycemia due to PCK1 deficiency (1) OMIM:[261680]
About this Structure
1NHX 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
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 Fri Feb 15 16:29:05 2008
Categories: Homo sapiens | Phosphoenolpyruvate carboxykinase (GTP) | Single protein | Dunten, P. | Foley, L.H. | Gubler, M.L. | Ramsey, G. | Wang, P. | Wertheimer, S.J. | EDO | FTB | MN | NA | PEP | Gluconeogenesis | Inhibitor | Xanthine
