General Information of Drug Therapeutic Target (DTT) (ID: TTIS4OW)

DTT Name Phosphodiesterase 8 (PDE8)
Synonyms High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Gene Name PDE8A
DTT Type
Patented-recorded target
[1]
BioChemical Class
Phosphoric diester hydrolase
UniProt ID
PDE8A_HUMAN
TTD ID
T05904
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.1.4.53
Sequence
MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
Function
May be involved in maintaining basal levels of the cyclic nucleotide and/or in the cAMP regulation of germ cell development. Binding to RAF1 reduces RAF1 'Ser-259' inhibitory-phosphorylation and stimulates RAF1-dependent EGF-activated ERK-signaling. Protects against cell death induced by hydrogen peroxide and staurosporine. Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
KEGG Pathway
Purine metabolism (hsa00230 )
Metabolic pathways (hsa01100 )
Cortisol synthesis and secretion (hsa04927 )
Cushing syndrome (hsa04934 )
Morphine addiction (hsa05032 )
Reactome Pathway
G alpha (s) signalling events (R-HSA-418555 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
6 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AC1M1SP5 DMEW5LD N. A. N. A. Patented [2]
BC11-28 DMTWIE2 N. A. N. A. Patented [2]
US8846654, 11 DMRUTJZ N. A. N. A. Patented [3]
US8846654, 251 DMML258 N. A. N. A. Patented [3]
US8846654, 294 DMP3RCH N. A. N. A. Patented [3]
US9493447, 1001 DM4MJ3U N. A. N. A. Patented [4]
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⏷ Show the Full List of 6 Patented Agent(s)
2 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-04957325 DMPEZKT Inflammation 1A00-CA43.1 Investigative [5]
PF-4957325-00 DMV4P7S Inflammation 1A00-CA43.1 Investigative [1]
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References

1 PDE8 regulates rapid Teff cell adhesion and proliferation independent of ICER. PLoS One. 2010 Aug 9;5(8):e12011.
2 Inhibitors of phosphodiesterase 11 (PDE11). US9173884.
3 Therapeutic applications in the cardiovascular field of quinazolinedione derivatives. US8846654.
4 Optically active PDE10 inhibitor. US9493447.
5 Differential Expression and Function of PDE8 and PDE4 in Effector T cells: Implications for PDE8 as a Drug Target in Inflammation.Front Pharmacol. 2016 Aug 23;7:259.