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

BRENDA support

Literature summary for 3.1.4.35 extracted from

  • Zhang, J.; Kuvelkar, R.; Wu, P.; Egan, R.W.; Billah, M.M.; Wang, P.
    Differential inhibitor sensitivity between human recombinant and native photoreceptor cGMP-phosphodiesterases (PDE6s) (2004), Biochem. Pharmacol., 68, 867-873.
    View publication on PubMed
Search for more literature for 3.1.4.35

Cloned(Commentary)

Cloned (Comment) Organism
cloning of rod PDE6 alpha and beta subunits and cone PDE6alpha', expression in Sf9 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
 Homo sapiens
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
-
 Homo sapiens
3-isobutyl-1-methylxanthine
-
 Homo sapiens
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
 Homo sapiens
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
-
 Homo sapiens
E4021
-
 Homo sapiens
additional information recombinant and native PDE6s exhibit differential sensitivity to inhibitors. This data caution the use of recombinant catalytic subunits of PDE6 in drug discovery or in structural/functional studies Homo sapiens
sildenafil
-
 Homo sapiens
zaprinast
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 recombinant and native
-

Source Tissue

Source Tissue Comment Organism Textmining
photoreceptor
-
 Homo sapiens
-
retinal cone
-
 Homo sapiens
-
retinal rod
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?

Synonyms

Synonyms Comment Organism
PDE6
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000026
-
 8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.0000035
-
 E4021 30°C, pH 7.4, native PDE6 Homo sapiens
0.0000036
-
 8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.0000173
-
 5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, native PDE6 Homo sapiens
0.0000183
-
 8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione 30°C, pH 7.4, native PDE6 Homo sapiens
0.0000245
-
 sildenafil 30°C, pH 7.4, native PDE6 Homo sapiens
0.0000487
-
 3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.0000546
-
 3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.0000936
-
 sildenafil 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.0000984
-
 sildenafil 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.0001014
-
 E4021 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.0001735
-
 E4021 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.000176
-
 2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, native PDE6 Homo sapiens
0.0001778
-
 zaprinast 30°C, pH 7.4, native PDE6 Homo sapiens
0.0003616
-
 2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.0006608
-
 2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.0007215
-
 3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione 30°C, pH 7.4, native PDE6 Homo sapiens
0.001206
-
 5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.001605
-
 5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one 30°C, pH 7.4, recombinant cone PDE6alpha' Homo sapiens
0.01145
-
 zaprinast 30°C, pH 7.4 cone PDE6alpha' Homo sapiens
0.01212
-
 3-isobutyl-1-methylxanthine 30°C, pH 7.4, native PDE6 Homo sapiens
0.01438
-
 zaprinast 30°C, pH 7.4 rod PDE6alphabeta Homo sapiens
0.06084
-
 3-isobutyl-1-methylxanthine 30°C, pH 7.4, recombinant rod PDE6alphabeta Homo sapiens
0.09485
-
 3-isobutyl-1-methylxanthine 30°C, pH 7.4, recombinant Homo sapiens