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CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach.

Abstract：

:We describe here a classical molecular modeling exercise that was carried out to provide a basis for the design of novel antagonist ligands of the CCR2 receptor. Using a theoretical model of the CCR2 receptor, docking studies were carried out to define plausible binding modes for the various known antagonist ligands, including our own series of indole piperidine compounds. On the basis of these results, a number of site-directed mutations (SDM) were designed that were intended to verify the proposed docking models. From these it was clear that further refinements would be necessary in the model. This was aided by the publication of a crystal structure of bovine rhodopsin, and a new receptor model was built by homology to this structure. This latest model enabled us to define ligand-docking hypotheses that were in complete agreement with the results of the SDM experiments.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Berkhout TA,Blaney FE,Bridges AM,Cooper DG,Forbes IT,Gribble AD,Groot PH,Hardy A,Ife RJ,Kaur R,Moores KE,Shillito H,Willetts J,Witherington J

doi

10.1021/jm030862l

keywords:

subject

Has Abstract

pub_date

2003-09-11 00:00:00

pages

4070-86

issue

19

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

杂志文章

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