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'''ENZYMATIC AND STRUCTURAL CHARACTERISATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES''' | '''ENZYMATIC AND STRUCTURAL CHARACTERISATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES''' | ||
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[[Category: Walkinshaw, M.]] | [[Category: Walkinshaw, M.]] | ||
[[Category: 3d-structure]] | [[Category: 3d-structure]] | ||
[[Category: | [[Category: Isomerase]] | ||
[[Category: | [[Category: Multigene family]] | ||
[[Category: Non peptide ligand]] | |||
[[Category: | [[Category: Rotamase]] | ||
[[Category: | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 13:18:32 2008'' | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | |||
Revision as of 10:18, 3 May 2008
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. 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 Sat May 3 13:18:32 2008
