Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T77400
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| Former ID |
TTDR00256
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| Target Name |
CGMP-dependent3',5'-cyclic phosphodiesterase
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| Gene Name |
PDE2A
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| Synonyms |
CGS-PDE; CGSPDE; Cyclic GMP stimulated phosphodiesterase; Cyclic-GMP phosphodiesterase; PDE-II; PDE2A
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| Target Type |
Clinical Trial
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| 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).
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| BioChemical Class |
Phosphoric diester hydrolases
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| Target Validation |
T77400
|
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| UniProt ID | |||||
| EC Number |
EC 3.1.4.17
|
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| Sequence |
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE |
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| Drugs and Mode of Action | |||||
| Drug(s) | CP-461 | Drug Info | Phase 2 | Inflammatory bowel disease | [1] |
| ND7001 | Drug Info | Phase 1 | Mood disorder | [2] | |
| IMAZODAN | Drug Info | Terminated | Discovery agent | [3] | |
| Inhibitor | (2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol | Drug Info | [4] | ||
| 2-Morpholin-4-yl-8-phenylethynyl-chromen-4-one | Drug Info | [5] | |||
| 3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione | Drug Info | [6] | |||
| 3-ISOBUTYL-1-METHYLXANTHINE | Drug Info | [7] | |||
| BAY-60-7550 | Drug Info | [4] | |||
| Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine | Drug Info | [8] | |||
| Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine | Drug Info | [8] | |||
| CP-461 | Drug Info | [9] | |||
| Cyclic Guanosine Monophosphate | Drug Info | [10] | |||
| EHNA | Drug Info | [11] | |||
| IMAZODAN | Drug Info | [12] | |||
| Modulator | ND7001 | Drug Info | [2] | ||
| 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 1 | ClinicalTrials.gov (NCT00060710) CP-461 in the Treatment of Patients With Advanced Melanoma. U.S. National Institutes of Health. | ||||
| REF 2 | Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures. Neurosignals. 2013;21(3-4):197-212. | ||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000379) | ||||
| REF 4 | J 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 5 | Bioorg Med Chem Lett. 2004 Jun 7;14(11):2847-51.PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues. | ||||
| REF 6 | J 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 7 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 8 | J 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 9 | Sulindac and its derivatives: a novel class of anticancer agents. Curr Opin Investig Drugs. 2001 May;2(5):677-83. | ||||
| REF 10 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 11 | Rapid 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 12 | J 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. | ||||
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