1w8v: Difference between revisions

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[[Image:1w8v.png|left|200px]]

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~~'''~~ENZYMATIC AND STRUCTURAL CHARACTERIZATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES~~'''~~

===ENZYMATIC AND STRUCTURAL CHARACTERIZATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES===

~~==Overview==~~

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~~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.

The line below this paragraph, {{ABSTRACT_PUBMED_14993672}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 14993672 is the PubMed ID number.

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==About this Structure==

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[[Category: Native high resolution]]

[[Category: Rotamase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 13~~:19:10 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:10:11 2008''

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-[[Image:1w8v.jpg|left|200px]]
+{{Seed}}
+[[Image:1w8v.png|left|200px]]
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 {{STRUCTURE_1w8v|  PDB=1w8v  |  SCENE=  }}
-'''ENZYMATIC AND STRUCTURAL CHARACTERIZATION OF NON PEPTIDE LIGAND CYCLOPHILIN COMPLEXES'''
+===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.
+The line below this paragraph, {{ABSTRACT_PUBMED_14993672}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 14993672 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_14993672}}
 ==About this Structure==
@@ Line 31: / Line 35: @@
 [[Category: Native high resolution]]
 [[Category: Rotamase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 13:19:10 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:10:11 2008''