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1w8m

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[[Image:1w8m.jpg|left|200px]]
[[Image:1w8m.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1w8m |SIZE=350|CAPTION= <scene name='initialview01'>1w8m</scene>, resolution 1.65&Aring;
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The line below this paragraph, containing "STRUCTURE_1w8m", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:E1p+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=E1P:ETHYL+OXO(PIPERIDIN-1-YL)ACETATE'>E1P</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1w8m| PDB=1w8m | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1w8m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1w8m OCA], [http://www.ebi.ac.uk/pdbsum/1w8m PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1w8m RCSB]</span>
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}}
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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]]
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[[Category: complex (isomerase/immunosuppressant)]]
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[[Category: Isomerase]]
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[[Category: isomerase]]
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[[Category: Multigene family]]
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[[Category: multigene family]]
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[[Category: Non peptide ligand]]
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[[Category: non peptide ligand]]
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[[Category: Rotamase]]
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[[Category: rotamase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 13:18:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:32:43 2008''
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Revision as of 10:18, 3 May 2008

Image:1w8m.jpg

Template:STRUCTURE 1w8m

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

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