1tou
From Proteopedia
| Line 7: | Line 7: | ||
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1tow|1TOW]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1tou FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1tou OCA], [http://www.ebi.ac.uk/pdbsum/1tou PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1tou RCSB]</span> | ||
}} | }} | ||
| Line 28: | Line 31: | ||
[[Category: Rondahl, L.]] | [[Category: Rondahl, L.]] | ||
[[Category: Uppenberg, J.]] | [[Category: Uppenberg, J.]] | ||
| - | [[Category: B1V]] | ||
[[Category: lipid-binding]] | [[Category: lipid-binding]] | ||
[[Category: transport]] | [[Category: transport]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:59:04 2008'' |
Revision as of 20:59, 30 March 2008
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| , resolution 2.00Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Related: | 1TOW
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal structure of human adipocyte fatty acid binding protein in complex with a non-covalent ligand
Overview
The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain length optimization led to novel compounds with low micromolar activity and good selectivity for human A-FABP.
About this Structure
1TOU is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors., Ringom R, Axen E, Uppenberg J, Lundback T, Rondahl L, Barf T, Bioorg Med Chem Lett. 2004 Sep 6;14(17):4449-52. PMID:15357970
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