1w8l
From Proteopedia
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==About this Structure== | ==About this Structure== | ||
| - | 1W8L is a | + | 1W8L 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 1P3 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Peptidylprolyl_isomerase Peptidylprolyl isomerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.2.1.8 5.2.1.8] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1W8L OCA]. |
==Reference== | ==Reference== | ||
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[[Category: rotamase]] | [[Category: rotamase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 15:07:46 2007'' |
Revision as of 13:02, 5 November 2007
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ENZYMATIC AND STRUCTURAL CHARACTERIZATION 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
1W8L is a Single protein structure of sequence from Homo sapiens with 1P3 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
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