1w8m
From Proteopedia
| Line 26: | Line 26: | ||
[[Category: rotamase]] | [[Category: rotamase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 19:48:05 2007'' |
Revision as of 17:41, 12 November 2007
|
ENZYMATIC AND STRUCTURAL CHARACTERISATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES
Overview
Piperidine ligands are described that provide the first examples of, non-peptidic ligand structures for the cyclophilin family of proteins., Crystal structures of two ligand complexes are compared with the, unliganded protein and show ligand-induced changes in side-chain, conformation and water binding. A peptidylprolyl cis-trans-isomerase assay, showed the dissociation constants of the two ligands to be 320 and 25 mM., This study also provides the first published data for both enzymatic, activity and three-dimensional structure for any protein-ligand complex, that binds with a high-millimolar dissociation constant. The structures, may be of relevance in the field of drug design, as they suggest starting, points for the design of larger tighter-binding analogues.
About this Structure
1W8M is a Single protein structure of sequence from Homo sapiens with E1P as ligand. Active as Peptidylprolyl isomerase, with EC number 5.2.1.8 Structure known Active Site: AC1. Full crystallographic information is available from OCA.
Reference
Enzymatic and structural characterization of non-peptide ligand-cyclophilin complexes., Kontopidis G, Taylor P, Walkinshaw MD, Acta Crystallogr D Biol Crystallogr. 2004 Mar;60(Pt 3):479-85. Epub 2004, Feb 25. PMID:14993672
Page seeded by OCA on Mon Nov 12 19:48:05 2007
