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

BRENDA support

Literature summary for 3.1.4.53 extracted from

  • Richter, W.; Unciuleac, L.; Hermsdorf, T.; Kronbach, T.; Dettmer, D.
    Identification of substrate specificity determinants in human cAMP-specific phosphodiesterase 4A by single-point mutagenesis (2001), Cell. Signal., 13, 159-167.
    View publication on PubMed
Search for more literature for 3.1.4.53

Cloned(Commentary)

Cloned (Comment) Organism
expressed in COS1 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
A590C mutation has no significant influence on substrate affinity or specificity Homo sapiens
D440A unlike wild type enzyme, the mutant enzyme shows activity with cGMP Homo sapiens
D440N unlike wild type enzyme, the mutant enzyme shows activity with cGMP Homo sapiens
F484Y mutation has no significant influence on substrate affinity or specificity Homo sapiens
L391A mutation has no significant influence on substrate affinity or specificity Homo sapiens
P595I mutation leads to 7fold decrease of substrate affinity and an 14fold decrease of the affinity towards the PDE4-specific inhibitor rolipram Homo sapiens
V501A mutation has no significant influence on substrate affinity or specificity Homo sapiens
W375Q mutation abolishes catalytic activity Homo sapiens
W605I mutation abolishes catalytic activity Homo sapiens
W605V mutation abolishes catalytic activity Homo sapiens
W605Y mutation abolishes catalytic activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-isobutyl-1-methyl-xanthine
-
 Homo sapiens
AWD 12-250
-
 Homo sapiens
AWD12-281
-
 Homo sapiens
cAMP-N1-oxide
-
 Homo sapiens
D-22888
-
 Homo sapiens
erythro-9-[3-(2-hydroxynonyl)]adenine 0.1 mM, 12% inhibition, wild-type enzyme Homo sapiens
LAS-31025
-
 Homo sapiens
Milrinone
-
 Homo sapiens
N6-Monobutyryl-cAMP
-
 Homo sapiens
N6-monobutyyl-cAMP
-
 Homo sapiens
quazinone 0.1 mM, 26% inhibition, wild-type enzyme Homo sapiens
rolipram
-
 Homo sapiens
RPR-73401
-
 Homo sapiens
sildenafil 0.1 mM, 29% inhibition, wild-type enzyme Homo sapiens
vinpocetine 0.1 mM, 34% inhibition Homo sapiens
zaprinast
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.002
-
 adenosine 3',5'-cyclic phosphate mutant enzyme L391A Homo sapiens
0.0032
-
 adenosine 3',5'-cyclic phosphate wild-type enzyme Homo sapiens
0.0038
-
 adenosine 3',5'-cyclic phosphate mutant enzyme F484Y Homo sapiens
0.0038
-
 adenosine 3',5'-cyclic phosphate mutant enzyme W375F Homo sapiens
0.0038
-
 adenosine 3',5'-cyclic phosphate mutant enzyme W605F Homo sapiens
0.0042
-
 adenosine 3',5'-cyclic phosphate mutant enzyme W375Y Homo sapiens
0.0044
-
 adenosine 3',5'-cyclic phosphate mutant enzyme V501A Homo sapiens
0.0069
-
 adenosine 3',5'-cyclic phosphate mutant enzyme D440A Homo sapiens
0.0074
-
 adenosine 3',5'-cyclic phosphate mutant enzyme A590C Homo sapiens
0.0164
-
 adenosine 3',5'-cyclic phosphate mutant enzyme D440N Homo sapiens
0.0244
-
 adenosine 3',5'-cyclic phosphate mutant enzyme P595I Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
adenosine 3',5'-cyclic phosphate + H2O
-
 Homo sapiens adenosine 5'-phosphate
-
 ?
additional information wild-type enzyme shows no activity with cGMP, mutant enzymes D440N and D440A show activity with cGMP Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
PDE4A
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
 wild-type enzyme Homo sapiens RPR-73401
0.000015
-
 wild-type enzyme Homo sapiens AWD12-281
0.00008
-
 wild-type enzyme Homo sapiens D-22888
0.000149
-
 mutant enzyme A590C Homo sapiens rolipram
0.000181
-
 wild-type enzyme Homo sapiens rolipram
0.0002
-
 mutant enzyme L391A Homo sapiens rolipram
0.000202
-
 mutant enzyme W375Y Homo sapiens rolipram
0.000256
-
 mutant enzyme V501A Homo sapiens rolipram
0.000293
-
 mutant enzyme W605F Homo sapiens rolipram
0.00032
-
 mutant enzyme F484Y Homo sapiens rolipram
0.0004
-
 mutant enzyme D440N Homo sapiens AWD 12-250
0.00245
-
 mutant enzyme P595I Homo sapiens rolipram
0.0033
-
 mutant enzyme D440N Homo sapiens Milrinone
0.00421
-
 wild-type enzyme Homo sapiens LAS-31025
0.0048
-
 mutant enzyme D440N Homo sapiens D-22888
0.00635
-
 wild-type enzyme Homo sapiens Milrinone
0.00728
-
 mutant enzyme D440N Homo sapiens LAS-31025
0.0097
-
 wild-type enzyme Homo sapiens AWD 12-250
0.0178
-
 mutant enzyme D440N Homo sapiens RPR-73401
0.0205
-
 mutant enzyme D440N Homo sapiens AWD12-281
0.0322
-
 wild-type enzyme Homo sapiens 3-isobutyl-1-methyl-xanthine
0.0395
-
 wild-type enzyme Homo sapiens sildenafil
0.04265
-
 mutant enzyme D440A Homo sapiens rolipram
0.0525
-
 mutant enzyme D440N Homo sapiens zaprinast
0.0861
-
 mutant enzyme D440N Homo sapiens sildenafil
0.08923
-
 mutant enzyme D440N Homo sapiens rolipram
0.175
-
 mutant enzyme D440N Homo sapiens 3-isobutyl-1-methyl-xanthine
0.18
-
 mutant enzyme W375F Homo sapiens rolipram
0.561
-
 wild-type enzyme Homo sapiens N6-monobutyyl-cAMP
1.13
-
 mutant enzyme D440N Homo sapiens N6-monobutyyl-cAMP
2.401
-
 wild-type enzyme Homo sapiens cAMP-N1-oxide
2.91
-
 mutant enzyme D440N Homo sapiens cAMP-N1-oxide