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1tow
From Proteopedia
(New page: 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" |
| - | <applet load="1tow" size=" | + | |
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 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
Categories: Homo sapiens | Single protein | Axen, E. | Barf, T. | Haile, S. | Lehmann, F. | Lundback, T. | Medina, C. | Rondahl, L. | Svensson, S. | Uppenberg, J. | CRZ | Lipid-binding | Transport
