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2h42

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[[Image:2h42.gif|left|200px]]
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{{STRUCTURE_2h42| PDB=2h42 | SCENE= }}
{{STRUCTURE_2h42| PDB=2h42 | SCENE= }}
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'''Crystal structure of PDE5 in complex with sildenafil'''
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===Crystal structure of PDE5 in complex with sildenafil===
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==Overview==
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Phosphodiesterase-5 (PDE5) is the target for sildenafil, vardenafil, and tadalafil, which are drugs for treatment of erectile dysfunction and pulmonary hypertension. We report here the crystal structures of a fully active catalytic domain of unliganded PDE5A1 and its complexes with sildenafil or icarisid II. These structures together with the PDE5A1-isobutyl-1-methylxanthine complex show that the H-loop (residues 660-683) at the active site of PDE5A1 has four different conformations and migrates 7-35A upon inhibitor binding. In addition, the conformation of sildenafil reported herein differs significantly from those in the previous structures of chimerically hybridized or almost inactive PDE5. Mutagenesis and kinetic analyses confirm that the H-loop is particularly important for substrate recognition and that invariant Gly(659), which immediately precedes the H-loop, is critical for optimal substrate affinity and catalytic activity.
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{{ABSTRACT_PUBMED_16735511}}
==About this Structure==
==About this Structure==
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[[Category: Pde5]]
[[Category: Pde5]]
[[Category: Viagra]]
[[Category: Viagra]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:50:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:49:58 2008''

Revision as of 00:50, 28 July 2008

Image:2h42.png

Template:STRUCTURE 2h42

Crystal structure of PDE5 in complex with sildenafil

Template:ABSTRACT PUBMED 16735511

About this Structure

2H42 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development., Wang H, Liu Y, Huai Q, Cai J, Zoraghi R, Francis SH, Corbin JD, Robinson H, Xin Z, Lin G, Ke H, J Biol Chem. 2006 Jul 28;281(30):21469-79. Epub 2006 May 30. PMID:16735511

Page seeded by OCA on Mon Jul 28 03:49:58 2008

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