2h44

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[[Image:2h44.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2h44| PDB=2h44 | SCENE= }}
{{STRUCTURE_2h44| PDB=2h44 | SCENE= }}
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'''Crystal structure of PDE5A1 in complex with icarisid II'''
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===Crystal structure of PDE5A1 in complex with icarisid II===
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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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The line below this paragraph, {{ABSTRACT_PUBMED_16735511}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16735511 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16735511}}
==About this Structure==
==About this Structure==
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[[Category: Icarisid ii]]
[[Category: Icarisid ii]]
[[Category: Pde5a inhibitor]]
[[Category: Pde5a inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:50:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 22:44:10 2008''

Revision as of 19:44, 27 July 2008

Image:2h44.png

Template:STRUCTURE 2h44

Crystal structure of PDE5A1 in complex with icarisid II

Template:ABSTRACT PUBMED 16735511

About this Structure

2H44 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

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