Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJGW1Z)

DTT Name Phosphodiesterase 2A (PDE2A)
Synonyms cGMP-dependent 3',5'-cyclic phosphodiesterase; PDE-II; Cyclic-GMP phosphodiesterase; Cyclic GMP-stimulated phosphodiesterase; Cyclic GMP stimulated phosphodiesterase; CGSPDE; CGS-PDE
Gene Name PDE2A
DTT Type
Clinical trial target
 [1]
Related Disease
Inborn purine/pyrimidine/nucleotide metabolism error [ICD-11: 5C55]
Indeterminate colitis [ICD-11: DD72]
Irritable bowel syndrome [ICD-11: DD91]
Mood disorder [ICD-11: 6A60-6E23]
BioChemical Class
Phosphoric diester hydrolase
UniProt ID
PDE2A_HUMAN
TTD ID
T77400
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
EC Number
EC 3.1.4.17
Sequence
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
Function
Plays an important role in growth and invasion of malignant melanoma cells (e. g. pseudomyxoma peritonei (PMP) cell line). Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
KEGG Pathway
Purine metabolism (hsa00230 )
cGMP-PKG signaling pathway (hsa04022 )
Morphine addiction (hsa05032 )
Reactome Pathway
G alpha (s) signalling events (R-HSA-418555 )
cGMP effects (R-HSA-418457 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CP-461 DMEYMTX Inflammatory bowel disease DD72 Phase 2 [1]
Tofisopam DMTGNWU Hyperuricaemia 5C55.Y Phase 2 [2]
ND7001 DMUBTC6 Mood disorder 6A60-6E23 Phase 1 [3]
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54 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
1,2,4-triazole [1,5-a]pyrimidin-7-yl derivative 1 DMQF62D N. A. N. A. Patented [4]
1,2,4-triazole [1,5-a]pyrimidin-7-yl derivative 2 DM8KWQ9 N. A. N. A. Patented [4]
1,2,4-triazole [1,5-a]pyrimidin-7-yl derivative 3 DMR1QP4 N. A. N. A. Patented [4]
1,2,4-triazole [4,3-a]quinoxaline derivative 1 DMD9QW2 N. A. N. A. Patented [4]
1,2,4-triazole [4,3-a]quinoxaline derivative 2 DM3DIW9 N. A. N. A. Patented [4]
1,2,4-triazole [4,3-a]quinoxaline derivative 3 DMKXRYM N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 1 DMWNKQ8 N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 2 DMU6ST7 N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 3 DM62K40 N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 4 DMQSTG9 N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 5 DM9E0ZD N. A. N. A. Patented [4]
1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivative 6 DM826JW N. A. N. A. Patented [4]
Benzodiazepine derivative 2 DM5ZGNK N. A. N. A. Patented [4]
Imidazo triazine derivative 1 DMLVY7A N. A. N. A. Patented [4]
Imidazo triazine derivative 2 DMZFG68 N. A. N. A. Patented [4]
Imidazo triazine derivative 3 DM142HI N. A. N. A. Patented [4]
Imidazo triazine derivative 4 DMZTS2O N. A. N. A. Patented [4]
Imidazo triazine derivative 5 DM18P4N N. A. N. A. Patented [4]
Imidazotriazinone derivative 1 DMX34PU N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 1 DMQBH81 N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 2 DMS3ROL N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 3 DMZ61T8 N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 4 DMKR5ZO N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 5 DM7UAKH N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 6 DMKRUAN N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 7 DMINBJM N. A. N. A. Patented [4]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 8 DM42EST N. A. N. A. Patented [4]
Imidazo[5,1-c][1,2,4]benzotriazine derivative 1 DMUB4QL N. A. N. A. Patented [4]
Imidazo[5,1-c][1,2,4]benzotriazine derivative 2 DMB8AJP N. A. N. A. Patented [4]
Imidazo[5,1-c][1,2,4]benzotriazine derivative 3 DMYX684 N. A. N. A. Patented [4]
Imidazo[5,1-c][1,2,4]benzotriazine derivative 4 DMWF4S7 N. A. N. A. Patented [4]
Oxindole derivative 1 DMMSVW5 N. A. N. A. Patented [4]
PMID27321640-Compound-58 DM0NYK3 N. A. N. A. Patented [4]
PMID27321640-Compound-59 DM41B5O N. A. N. A. Patented [4]
PMID27321640-Compound-74 DMHWV67 N. A. N. A. Patented [4]
PMID27321640-Compound-75 DM2P5J9 N. A. N. A. Patented [4]
PMID27321640-Compound-76 DM40LIN N. A. N. A. Patented [4]
Purin-6-one derivative 1 DM92SWJ N. A. N. A. Patented [4]
Pyrazolo[3,4-d]pyrimidine derivative 1 DMT57C4 N. A. N. A. Patented [4]
Pyrazolo[3,4-d]pyrimidine derivative 2 DMO054V N. A. N. A. Patented [4]
Pyrazolo[3,4-d]pyrimidine derivative 3 DMRKVP9 N. A. N. A. Patented [4]
Pyrazolo[3,4-d]pyrimidine derivative 4 DMGFAS6 N. A. N. A. Patented [4]
Pyrido[1,2,4]triazolo[4,3-a]pyrazine derivative 1 DMHKRVL N. A. N. A. Patented [4]
Pyrido[1,2,4]triazolo[4,3-a]pyrazine derivative 2 DMUO25Y N. A. N. A. Patented [4]
Pyrido[1,2,4]triazolo[4,3-a]pyrazine derivative 3 DMAEYNT N. A. N. A. Patented [4]
Pyrido[2,3-d]pyrimidine-2,4-diamine derivative 1 DMM8CL4 N. A. N. A. Patented [4]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 1 DMC8935 N. A. N. A. Patented [4]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 2 DM4CSBD N. A. N. A. Patented [4]
Triazolo-phthalazine derivative 1 DMU9A7V N. A. N. A. Patented [4]
Triazolo-pyridine derivative 2 DMXPQ24 N. A. N. A. Patented [4]
Triazolo-pyridine derivative 3 DMQL1TV N. A. N. A. Patented [4]
Triazolo-pyridine derivative 4 DM5ZQKS N. A. N. A. Patented [4]
Triazolo-pyridine derivative 5 DM1R205 N. A. N. A. Patented [4]
Triazolo-pyridine derivative 6 DMX4WFP N. A. N. A. Patented [4]
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⏷ Show the Full List of 54 Patented Agent(s)
1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
IMAZODAN DMWTFO3 N. A. N. A. Terminated [5]
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8 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(2R,3S)-3-(6-Amino-purin-9-yl)-nonan-2-ol DM852Z6 Discovery agent N.A. Investigative [6]
2-Morpholin-4-yl-8-phenylethynyl-chromen-4-one DMNKHOI Discovery agent N.A. Investigative [7]
BAY-60-7550 DMQZ7JD Discovery agent N.A. Investigative [6]
Benzyl-(2-pyridin-3-yl-quinazolin-4-yl)-amine DMYDGCI Discovery agent N.A. Investigative [8]
Benzyl-(2-pyridin-4-yl-quinazolin-4-yl)-amine DMESVWC Discovery agent N.A. Investigative [8]
Cyclic guanosine monophosphate DMOU93V Discovery agent N.A. Investigative [9]
EHNA DM014WS Discovery agent N.A. Investigative [10]
isobutylmethylxanthine DM46F5X Discovery agent N.A. Investigative [11], [12]
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⏷ Show the Full List of 8 Investigative Drug(s)

References

1 Sulindac and its derivatives: a novel class of anticancer agents. Curr Opin Investig Drugs. 2001 May;2(5):677-83.
2 The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25.
3 Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures. Neurosignals. 2013;21(3-4):197-212.
4 Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2016 Aug;26(8):933-46.
5 Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of conges... J Med Chem. 1984 Sep;27(9):1099-101.
6 The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. J Med Chem. 2005 May 19;48(10):3449-62.
7 PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2847-51.
8 Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and th... J Med Chem. 1995 Sep 1;38(18):3547-57.
9 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
10 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.
11 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
12 A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. J Med Chem. 1985 May;28(5):537-45.