1tow: Difference between revisions
New page: left|200px<br /> <applet load="1tow" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tow, resolution 2.00Å" /> '''Crystal structure o... |
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[[Image:1tow.gif|left|200px]]<br /> | [[Image:1tow.gif|left|200px]]<br /><applet load="1tow" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1tow, resolution 2.00Å" /> | caption="1tow, resolution 2.00Å" /> | ||
'''Crystal structure of human adipocyte fatty acid binding protein in complex with a carboxylic acid ligand'''<br /> | '''Crystal structure of human adipocyte fatty acid binding protein in complex with a carboxylic acid ligand'''<br /> | ||
==Overview== | ==Overview== | ||
Low micromolar human A-FABP inhibitors were found by utilizing a | Low micromolar human A-FABP inhibitors were found by utilizing a fluorescence polarization assay, X-ray crystallography and modeling. The carbazole- and indole-based inhibitors displayed approximately 10-fold preferences over human H-FABP and E-FABP, and are highly selective against I-FABP. This communication describes the SAR for drug-like synthetic inhibitors of human A-FABP. | ||
==About this Structure== | ==About this Structure== | ||
1TOW 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 CRZ as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1TOW 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=CRZ:'>CRZ</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TOW OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transport]] | [[Category: transport]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:15:54 2008'' | ||
Revision as of 13:15, 21 February 2008
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Crystal structure of human adipocyte fatty acid binding protein in complex with a carboxylic acid ligand
Overview
Low micromolar human A-FABP inhibitors were found by utilizing a fluorescence polarization assay, X-ray crystallography and modeling. The carbazole- and indole-based inhibitors displayed approximately 10-fold preferences over human H-FABP and E-FABP, and are highly selective against I-FABP. This communication describes the SAR for drug-like synthetic inhibitors of human A-FABP.
About this Structure
1TOW is a Single protein structure of sequence from Homo sapiens with CRZ as ligand. Full crystallographic information is available from OCA.
Reference
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target., Lehmann F, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Lundback T, Rondahl L, Barf T, Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8. PMID:15357969
Page seeded by OCA on Thu Feb 21 15:15:54 2008
