1tou
From Proteopedia
(New page: 200px<br /> <applet load="1tou" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tou, resolution 2.00Å" /> '''Crystal structure o...) |
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| - | [[Image:1tou.gif|left|200px]]<br /> | + | [[Image:1tou.gif|left|200px]]<br /><applet load="1tou" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1tou" size=" | + | |
caption="1tou, resolution 2.00Å" /> | caption="1tou, resolution 2.00Å" /> | ||
'''Crystal structure of human adipocyte fatty acid binding protein in complex with a non-covalent ligand'''<br /> | '''Crystal structure of human adipocyte fatty acid binding protein in complex with a non-covalent ligand'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The synthesis and biological evaluation of novel human A-FABP inhibitors | + | 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== | ==About this Structure== | ||
| - | 1TOU 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 B1V as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1TOU 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=B1V:'>B1V</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TOU 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 15:15:48 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 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 with as ligand. 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
Page seeded by OCA on Thu Feb 21 15:15:48 2008
Categories: Homo sapiens | Single protein | Axen, E. | Barf, T. | Lundback, T. | Ringom, R. | Rondahl, L. | Uppenberg, J. | B1V | Lipid-binding | Transport
