Therapeutic Targets Database
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TTD Target ID: TTDS00390

Target Information
NameCGMP-inhibited 3',5'-cyclic phosphodiesterase A    
Type of targetSuccessful target    
SynonymsCGI-PDE A    
Cyclic GMP inhibited phosphodiesterase A    
Phosphodiesterase 3A    
DiseaseBronchial asthma
[ICD9: 493   ICD10: J45]
[1]
Chronic myeloid leukemia
[ICD9: 205.1   ICD10: C92.1]
[2]
Vascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[3]
Drug(s)AminophyllineApprovedBronchial asthma[4][5]
AnagrelideApprovedThrombocythemia[6]
CilostazolApprovedIntermittent claudication[7][3][8]
MilrinoneApprovedCongestive heart failure[9]
BioChemical ClassHydrolases acting on ester bonds    
EC NumberEC 3.1.4.17
PathwayInsulin signaling pathway
Purine metabolism
UniProt IDQ14432
PDB Structure1LRC.    
FunctionHydrolyzes both cyclic amp (camp) and cyclic gmp (cgmp) (by similarity).    
SequenceMAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRK LSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAP GGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGV GEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYL AYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEM SGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDL LADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLA IPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWN NPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVS KISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADE PLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYA PETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFE DMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVIN DHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDH PGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFL VIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKEL HLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAG LMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLL QNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPD Q
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,3,9,9a-Tetrahydro-imidazo[4,5-b]quinolin-2-one[10]
1,3-Dihydro-imidazo[4,5-b]quinolin-2-one[10]
1,3-Dihydro-naphtho[2,3-d]imidazol-2-one[10]
1,5-Dihydro-imidazo[2,1-b]quinazolin-2-one[11]
2-morpholino-7- (2-phenylethynyl)-4H-chromen-4-one[12]
2-morpholino-7-phenyl-4H-chromen-4-one[12]
2-morpholino-8- (2-phenylethynyl)-4H-chromen-4-one[12]
3-Isobutyl-1-methyl-3,7-dihydro-purine-2,6-dione[13]
5-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
6- (2-Imidazol-1-yl-vinyl)-1H-quinolin-2-one[14]
6-Imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one[14]
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one[14]
7-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
7-Ethoxy-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
7-Fluoro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
7-Iodo-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one[11]
7-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
8-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
8-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one[10]
8-methyl-2-morpholino-7-phenoxy-4H-chromen-4-one[12]
8-methyl-2-morpholino-7-phenyl-4H-chromen-4-one[12]
Aminophylline[4][5]
Anagrelide[6]
BENZOYLENUREA[15]
BMY-20844[16]
CI-930[17]
Cilostazol[7][3][8]
FENOXIMONE[18]
IMAZODAN[14]
KURAIDIN[19]
KURARINOL[19]
Milrinone[9]
OPC-13013[13]
RO-201724[13]
SOPHOFLAVESCENOL[19]
TETRAHYDROBENXIMIDAZOLE[17]
VESNARINONE[20]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Novel chronotherapeutic rectal aminophylline delivery system for therapy of asthma. Int J Pharm. 2009 Jun 23. [Epub ahead of print] To Reference
Ref 2Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase. Vnitr Lek. 2006 Sep;52(9):819-22. To Reference
Ref 3The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. To Reference
Ref 4Topical fat reduction from the waist. Diabetes Obes Metab. 2007 May;9(3):300-3. To Reference
Ref 5Spasmolytic effects of colforsin daropate on serotonin-induced pulmonary hypertension and bronchoconstriction in dogs. Acta Anaesthesiol Scand. 2002 Mar;46(3):297-302. To Reference
Ref 6Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med. 2005 Jul 7;353(1):33-45. To Reference
Ref 7Cilostazol: therapeutic potential against focal cerebral ischemic damage. Curr Pharm Des. 2006;12(5):565-73. To Reference
Ref 8Randomized comparison of cilostazol versus ticlopidine hydrochloride for antiplatelet therapy after coronary stent implantation for prevention of late restenosis. Am Heart J. 2002 Aug;144(2):303-8. To Reference
Ref 9Milrinone inhibits hypoxia or hydrogen dioxide-induced persistent sodium current in ventricular myocytes. Eur J Pharmacol. 2009 Aug 15;616(1-3):206-12. Epub 2009 Jun 21. To Reference
Ref 10J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation. To Reference
Ref 11J Med Chem. 1988 Nov;31(11):2136-45.Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline. To Reference
Ref 12Bioorg Med Chem Lett. 2006 Feb 15;16(4):969-73. Epub 2005 Nov 15.Analysis of anti-PDE3 activity of 2-morpholinochromone derivatives reveals multiple mechanisms of anti-platelet activity. To Reference
Ref 13J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. To Reference
Ref 14J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. To Reference
Ref 15Eur J Med Chem. 2008 Jul;43(7):1349-59. Epub 2007 Dec 21.CODES, a novel procedure for ligand-based virtual screening: PDE7 inhibitors as an application example. To Reference
Ref 16J Med Chem. 1992 Jul 10;35(14):2688-96.Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility. To Reference
Ref 17J Med Chem. 1989 Feb;32(2):342-50.Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure. To Reference
Ref 18J Med Chem. 1987 Feb;30(2):303-18.Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856). To Reference
Ref 19Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. To Reference
Ref 20Bioorg Med Chem. 2010 Jan 15;18(2):855-62. Epub 2009 Nov 26.Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors. To Reference



 

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