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Sandbox Reserved 1127

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== Function ==
== Function ==
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Human PDE5 is the 5th isoform of the 12 known phosphodiesterases. This enzymes family is responsible for the hydrolysis of cGMP and cAMP into GMP and AMP. PDE5 specifically catalyses cGMP hydrolysis into 5'GMP. The cGMP is an usual second messager in cell signalling pathways, like NO synthesis. By degradating nucleotides, this enzyme of class I regulates the cGMP concentration in the organism by an allosteric regulation system.
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PDE5 is an phosphodiesterase : this enzyme catalyzes the hydrolysis of cGMP into 5'GMP. CGMP is an usual second messager in cell transduction. PDE5 regulates its concentration by hydrolysis.
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Human PDE5 is a PDE of class I.
PDE5 function affects the smooth muscle, blood vessels or penis, uterus and intestines.
PDE5 function affects the smooth muscle, blood vessels or penis, uterus and intestines.
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acylation : K364.
acylation : K364.
ubiquitinylation : K714.
ubiquitinylation : K714.
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The ubiquitinylation of <scene name='71/719868/K714/1'>K714</scene> (in fushia) and the phosphorylation of are involved in the binding of cGMP to PDE5 catalytic domain.
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The ubiquitinylation of <scene name='71/719868/K714/1'>K714</scene> (in fushia) and the phosphorylation of <scene name='71/719868/S869/1'>S869</scene> (in yellow) are present in the catalytic site and the phosphorylation of S819 is involved in cGMP binding.
== Inhibitors and medical application ==
== Inhibitors and medical application ==
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Inhibitors of PDE5 prevent cGMP from binding the catalytic site by competititve inhibition. They have more affinity for this domain than cGMP.
Inhibitors of PDE5 prevent cGMP from binding the catalytic site by competititve inhibition. They have more affinity for this domain than cGMP.
Sildenafil (active substance of Viagra) binds to PDE5 catalytic domain through:
Sildenafil (active substance of Viagra) binds to PDE5 catalytic domain through:
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hydrogen bonds made between Gln775 and Gln817 of PDE5 (green) and <scene name='71/719868/Sildenafil/1'>Sildenafil</scene> (red)
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**hydrogen bonds made between Gln775 and Gln817 of PDE5 (green) and <scene name='71/719868/Sildenafil/1'>Sildenafil</scene> (red)
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coordination bond made with
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**coordination bond made with <scene name='71/719868/Mg/1'>Mg2+</scene> in catalytic site
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coordination made with
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**coordination made with <scene name='71/719868/Zn/1'>Zn2+</scene> in catalytic site

Revision as of 17:35, 30 January 2016

This Sandbox is Reserved from 15/12/2015, through 15/06/2016 for use in the course "Structural Biology" taught by Bruno Kieffer at the University of Strasbourg, ESBS. This reservation includes Sandbox Reserved 1120 through Sandbox Reserved 1159.
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Human PDE5

PDE5 and its inhibitor Sildenafil

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References

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