Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.1.4.35 extracted from

  • Sung, B.J.; Hwang, K.Y.; Jeon, Y.H.; Lee, J.I.; Heo, Y.S.; Kim, J.H.; Moon, J.; Yoon, J.M.; Hyun, Y.L.; Kim, E.; Eum, S.J.; Park, S.Y.; Lee, J.O.; Lee, T.G.; Ro, S.; Cho, J.M.
    Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules (2003), Nature, 425, 98-102.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of the catalytic domain of PDE5A1 in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystals of PDE5A1 complexed with the inhibitors sildenafil, tadalafil or vardenafil, PDE5A1-inhibitor complex crystals are grown at 4°C by hanging-drop vapour diffusion, adding 0.001 ml protein solution containing 10 mg/ml protein in 25 mM Tris-HCl, pH 7.5, 100 mM NaCl and 5 mM dithiothreitol, to 0.001 ml well solution consisting of 100 mM Tris-HCl, pH 7.2-7.5, 200 mM MgCl2 and 6-9% polyethylene glycol 8000, crystals diffract to 2.3-2.8 A Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate trivial name sildenafil citrate or Viagra Homo sapiens
2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one trivial name vardenafil or Levitra Homo sapiens
6-benzo[1,3]dioxol-5-yl-2-methyl-2,3,6,7,12,12a-hexahydropyrazinol[1',2':1,6]pyrido[3,4-b]indole-1,4-dione trivial name tadalafil or Cialis Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
guanosine 3',5'-cyclic phosphate + H2O Homo sapiens
-
guanosine 5'-phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens O76074
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant catalytic domain of PDE5A1 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
corpus cavernosum
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
guanosine 3',5'-cyclic phosphate + H2O
-
Homo sapiens guanosine 5'-phosphate
-
?

Synonyms

Synonyms Comment Organism
cGMP-specific PDE5
-
Homo sapiens
PDE5A1
-
Homo sapiens
phosphodiesterase 5
-
Homo sapiens