Target Information

Target General Infomation
Target ID
T77400
Former ID
TTDR00256
Target Name
CGMP-dependent3',5'-cyclic phosphodiesterase
Gene Name
PDE2A
Synonyms
CGS-PDE; CGSPDE; Cyclic GMP stimulated phosphodiesterase; Cyclic-GMP phosphodiesterase; PDE-II; PDE2A
Target Type
Clinical Trial
Disease Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Mood disorder [ICD10: F30-F39]
Function
Hydrolyzes both cyclic amp (camp) and cyclic gmp (cgmp).
BioChemical Class
Phosphoric diester hydrolases
Target Validation
T77400
UniProt ID
O00408
EC Number
EC 3.1.4.17
Sequence
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
Drugs and Mode of Action
Drug(s) CP-461 Drug Info Phase 2 Inflammatory bowel disease [521555]
ND7001 Drug Info Phase 1 Mood disorder [532028]
IMAZODAN Drug Info Terminated Discovery agent [544637]
Inhibitor (2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol Drug Info [527549]
2-Morpholin-4-yl-8-phenylethynyl-chromen-4-one Drug Info [527068]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info [533395]
3-ISOBUTYL-1-METHYLXANTHINE Drug Info [551374]
BAY-60-7550 Drug Info [527549]
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine Drug Info [533684]
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine Drug Info [533684]
CP-461 Drug Info [535265]
Cyclic Guanosine Monophosphate Drug Info [551393]
EHNA Drug Info [534171]
IMAZODAN Drug Info [533555]
Modulator ND7001 Drug Info [532028]
Pathways
KEGG Pathway Purine metabolism
cGMP-PKG signaling pathway
Morphine addiction
NetPath Pathway TSH Signaling Pathway
Reactome cGMP effects
G alpha (s) signalling events
References
Ref 521555ClinicalTrials.gov (NCT00060710) CP-461 in the Treatment of Patients With Advanced Melanoma. U.S. National Institutes of Health.
Ref 532028Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures. Neurosignals. 2013;21(3-4):197-212.
Ref 544637Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000379)
Ref 527068Bioorg Med Chem Lett. 2004 Jun 7;14(11):2847-51.PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues.
Ref 527549J Med Chem. 2005 May 19;48(10):3449-62.The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
Ref 532028Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures. Neurosignals. 2013;21(3-4):197-212.
Ref 533395J 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.
Ref 533555J Med Chem. 1984 Sep;27(9):1099-101.Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.
Ref 533684J Med Chem. 1995 Sep 1;38(18):3547-57.Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Ref 534171Rapid regulation of PDE-2 and PDE-4 cyclic AMP phosphodiesterase activity following ligation of the T cell antigen receptor on thymocytes: analysis using the selective inhibitors erythro-9-(2-hydroxy-3-nonyl)-adenine (EHNA) and rolipram. Cell Signal. 1996 Feb;8(2):97-110.
Ref 535265Sulindac and its derivatives: a novel class of anticancer agents. Curr Opin Investig Drugs. 2001 May;2(5):677-83.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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