2gmv: Difference between revisions
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New page: left|200px<br /> <applet load="2gmv" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gmv, resolution 2.30Å" /> '''PEPCK complex with ... |
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[[Image:2gmv.gif|left|200px]]<br /> | [[Image:2gmv.gif|left|200px]]<br /><applet load="2gmv" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2gmv" size=" | |||
caption="2gmv, resolution 2.30Å" /> | caption="2gmv, resolution 2.30Å" /> | ||
'''PEPCK complex with a GTP-competitive inhibitor'''<br /> | '''PEPCK complex with a GTP-competitive inhibitor'''<br /> | ||
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==Overview== | ==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. | 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. | ||
==About this Structure== | ==About this Structure== | ||
2GMV 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, PEP and UN8 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:// | 2GMV 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=PEP:'>PEP</scene> and <scene name='pdbligand=UN8:'>UN8</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=2GMV OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: xanthine]] | [[Category: xanthine]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:55:54 2008'' | ||
