This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
1w8m
From Proteopedia
| Line 1: | Line 1: | ||
| - | [[Image:1w8m.jpg|left|200px]] | + | [[Image:1w8m.jpg|left|200px]] |
| - | + | ||
| - | '''ENZYMATIC AND STRUCTURAL CHARACTERISATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES''' | + | {{Structure |
| + | |PDB= 1w8m |SIZE=350|CAPTION= <scene name='initialview01'>1w8m</scene>, resolution 1.65Å | ||
| + | |SITE= <scene name='pdbsite=AC1:E1p+Binding+Site+For+Chain+A'>AC1</scene> | ||
| + | |LIGAND= <scene name='pdbligand=E1P:ETHYL OXO(PIPERIDIN-1-YL)ACETATE'>E1P</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''ENZYMATIC AND STRUCTURAL CHARACTERISATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES''' | ||
| + | |||
==Overview== | ==Overview== | ||
| Line 7: | Line 16: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1W8M is a [ | + | 1W8M is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1W8M OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/14993672 14993672] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Peptidylprolyl isomerase]] | [[Category: Peptidylprolyl isomerase]] | ||
| Line 25: | Line 34: | ||
[[Category: rotamase]] | [[Category: rotamase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:53:46 2008'' |
Revision as of 12:53, 20 March 2008
| |||||||
| , resolution 1.65Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | |||||||
| Activity: | Peptidylprolyl isomerase, with EC number 5.2.1.8 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Thu Mar 20 14:53:46 2008
