2h44

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[[Image:2h44.gif|left|200px]]
[[Image:2h44.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2h44 |SIZE=350|CAPTION= <scene name='initialview01'>2h44</scene>, resolution 1.8&Aring;
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The line below this paragraph, containing "STRUCTURE_2h44", creates the "Structure Box" on the page.
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|SITE=
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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=7CA:5,7-DIHYDROXY-2-(4-METHOXYPHENYL)-8-(3-METHYLBUTYL)-4-OXO-4H-CHROMEN-3-YL+6-DEOXY-ALPHA-L-MANNOPYRANOSIDE'>7CA</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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/3',5'-cyclic-GMP_phosphodiesterase 3',5'-cyclic-GMP phosphodiesterase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.4.35 3.1.4.35] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PDE5A, PDE5 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2h44| PDB=2h44 | SCENE= }}
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|RELATEDENTRY=[[2h40|2H40]], [[2h42|2H42]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2h44 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2h44 OCA], [http://www.ebi.ac.uk/pdbsum/2h44 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2h44 RCSB]</span>
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}}
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'''Crystal structure of PDE5A1 in complex with icarisid II'''
'''Crystal structure of PDE5A1 in complex with icarisid II'''
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[[Category: Ke, H.]]
[[Category: Ke, H.]]
[[Category: Wang, H.]]
[[Category: Wang, H.]]
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[[Category: flavonoid]]
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[[Category: Flavonoid]]
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[[Category: icarisid ii]]
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[[Category: Icarisid ii]]
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[[Category: pde5a inhibitor]]
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[[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 Mon Mar 31 03:25:10 2008''
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Revision as of 02:50, 4 May 2008

Image:2h44.gif

Template:STRUCTURE 2h44

Crystal structure of PDE5A1 in complex with icarisid II


Overview

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.

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 Page seeded by OCA on Sun May 4 05:50:46 2008

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