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Drug-Target Interaction

Drug

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PubChem ID:2754
Structure:
Synonyms:
2(1H)-Quinolinone,
2(1H)-Quinolinone, 3,4-dihydro-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-
2(1H)-Quionlinone, 6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-
3,4-Dihydro-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone
6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone
6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril
6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxyl)-3,4-dihydrocarobostyril
6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone
6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
73963-72-1
89332-50-3
BRN 3632107
BSPBio_002759
C045645
C0737_SIGMA
C20H27N5O2
CHEBI:31401
CILOSTAZOL
Cilostazol (JP15/USAN/INN)
Cilostazol [INN:JAN]
Cilostazole
Cilostazolum
Cilostazolum [INN-Latin]
CPD000058428
D01896
DB01166
EU-0100218
KBio3_002259
KBioGR_001184
Lopac-C-0737
Lopac0_000218
LS-142693
MLS000028470
MLS000758281
MLS000759507
MLS001076067
MLS002153891
NCGC00015207-01
NCGC00015207-02
NCGC00022153-02
NCGC00022153-04
NCGC00022153-05
NCGC00022153-06
NCGC00022153-07
OPC 13013
OPC 21
OPC-13013
OPC-21
Otsuka brand of cilostazol
Pharmacia brand of cilostazol
Pletaal
Pletal
Pletal (TN)
Pletal, Cilostazol
SAM001246734
SAM001247085
SMR000058428
SPBio_001256
SPECTRUM1505230
Spectrum2_001118
Spectrum3_001170
Spectrum4_000772
Spectrum5_001762
ST5408866
TL8005113
Tocris-1692
ZINC01552174

Target

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Uniprot ID:PDE3A_HUMAN
Synonyms:
CGI-PDE A
cGMP-inhibited 3',5'-cyclic phosphodiesterase A
Cyclic GMP-inhibited phosphodiesterase A
EC-Numbers:3.1.4.17
Organism:Homo sapiens
Human
PDB IDs:1LRC
Structure:
1LRC

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----

References:

17392505
Thrombin regulates intracellular cyclic AMP concentration in human platelets through phosphorylation/activation of phosphodiesterase 3A.. Wei Zhang; Robert W Colman (2007) Blood display abstract
Thrombin-induced cyclic AMP (cAMP) reduction potentates several steps in platelet activation, including Ca(++) mobilization, cytoskeletal reorganization, and fibrinogen receptor conformation. We now reinvestigate the signaling pathways by which intracellular cAMP content is controlled after platelet activation by thrombin. When washed human platelets were stimulated with thrombin, cAMP-dependent phosphodiesterase (PDE3A) activity was significantly increased. A nonselective PDE inhibitor, 3-isobutyl-1-methylxanthine (IBMX), and the PDE3 selective inhibitors milrinone and cilostazol each suppressed thrombin-induced cAMP-dependent PDE responses, but not 2 different PDE2 inhibitors. Selective inhibition of PDE3A resulted in reversal of thrombin-induced cAMP reduction, indicating that thrombin activated PDE3A. In synergy with inhibition of adenylate cyclase by thrombin, activated PDE3A accelerates cAMP hydrolysis and maximally reduces the cAMP content. Thrombin-induced PDE3A activation was diminished concomitantly with dephosphorylation of PDE3A by protein phosphatase 1 (PP1). An Akt inhibitor blocked PDE3A activation and constrained thrombin-induced cAMP reduction. A P2Y(12) inhibitor also reduced thrombin-induced cAMP reduction. The combination of both reversed cAMP decrease by thrombin. Thrombin-mediated phosphorylated PDE3A was isolated by liquid chromatography, detected by a monoclonal antibody against Akt-phosphorylated substrate, and verified by immunoprecipitation study. The predominant isoform phosphorylated by Akt was the 136-kDa species. We suggest that activation/phosphorylation of PDE3A via Akt signaling pathway participates in regulating cAMP during thrombin activation of platelets.
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