Sandbox Reserved 957: Difference between revisions
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== Inhibition == | == Inhibition == | ||
In the treatment erection dysfunction, the inhibitors Sildenafil, Vardenafil and Tadalafil are used, like in the pulmonary hypertension<ref>[6]</ref>. Sildenafil may cure sleeping trouble after a intercontinental travel <ref>[11]</ref>, may help to recover neural liaisons after an injury (the motor function<ref>[12]</ref> and the sensory motor function<ref>[13]</ref>) and can be vascular effects.<br \> | In the treatment erection dysfunction, the inhibitors Sildenafil, Vardenafil and Tadalafil are used, like in the pulmonary hypertension<ref>[6]</ref>. Sildenafil may cure sleeping trouble after a intercontinental travel <ref>[11]</ref>, may help to recover neural liaisons after an injury (the motor function<ref>[12]</ref> and the sensory motor function<ref>[13]</ref>) and can be vascular effects.<br \> | ||
<gallery>Image:Sildenafil.jpg | <gallery caption="The Sildenafil">Image:Sildenafil.jpg|Sildenafil Inhibitor, R1 in blue, R2 in green and R3 in red | ||
Image:Sildenafilspace.jpg | Image:Sildenafilspace.jpg|Sildenafil Inhibitor in the space in the enzyme</gallery> | ||
* PDE5 inhibitors might help physical condition in Duchene muscular dystrophy<ref>[14]</ref>, improve of cognitive function <ref>[9]</ref>and have antidepressant effect<ref>[10]</ref> , also they might have an artero<ref>[15]</ref> and endothelial cell protective effect<ref>[16]</ref> so they have cardiac protection effect<ref>[17]</ref> (controversial, cf. clinical trial “RELAX”), finally they slow tumer cell growth (Tadalafil-like)<ref>[18]</ref><br \> | * PDE5 inhibitors might help physical condition in Duchene muscular dystrophy<ref>[14]</ref>, improve of cognitive function <ref>[9]</ref>and have antidepressant effect<ref>[10]</ref> , also they might have an artero<ref>[15]</ref> and endothelial cell protective effect<ref>[16]</ref> so they have cardiac protection effect<ref>[17]</ref> (controversial, cf. clinical trial “RELAX”), finally they slow tumer cell growth (Tadalafil-like)<ref>[18]</ref><br \> | ||
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* 3 parts (R1: pyrazolopyrimidinone group; R2: ethoxyphenyl; R3: methylpiperazine)<br \> | * 3 parts (R1: pyrazolopyrimidinone group; R2: ethoxyphenyl; R3: methylpiperazine)<br \> | ||
* It is bound near Metallic ions but does not interact with them.<br \> | * It is bound near Metallic ions but does not interact with them.<br \> | ||
{{Clr}} | |||
Binding amino acid for the Sildenafil:<br \> | Binding amino acid for the Sildenafil:<br \> | ||
* R1 group have contacts with <scene name='60/604476/R1-1/1'>Gln817</scene> (2 hydrogen bounds, so it increases Sildenafil affinity), <scene name='60/604476/R1-1/1'>Phe820</scene> (Sildenafil stacks against it), <scene name='60/604476/R1-1/1'>Try612</scene> (hydrogen bound so it increases Sildenafil affinity <ref>[24]</ref>), <scene name='60/604476/R1-1/1'>Leu765</scene> and <scene name='60/604476/R1-1/1'>Ala767</scene> <ref>[21]</ref>. And there is hydrophobic interactions between the pyrazol ring and residues <scene name='60/604476/R1-2/1'>Val782, Leu785, Tyr612 and Phe820</scene> <ref>[24]</ref>.<br \> | * R1 group have contacts with <scene name='60/604476/R1-1/1'>Gln817</scene> (2 hydrogen bounds, so it increases Sildenafil affinity), <scene name='60/604476/R1-1/1'>Phe820</scene> (Sildenafil stacks against it), <scene name='60/604476/R1-1/1'>Try612</scene> (hydrogen bound so it increases Sildenafil affinity <ref>[24]</ref>), <scene name='60/604476/R1-1/1'>Leu765</scene> and <scene name='60/604476/R1-1/1'>Ala767</scene> <ref>[21]</ref>. And there is hydrophobic interactions between the pyrazol ring and residues <scene name='60/604476/R1-2/1'>Val782, Leu785, Tyr612 and Phe820</scene> <ref>[24]</ref>.<br \> | ||