General Information of Drug Therapeutic Target (DTT) (ID: TTFLH0E)

DTT Name Serine/threonine PP1-alpha (PPP1CA)
Synonyms Serine/threonine-protein phosphatase PP1-alpha catalytic subunit; Protein phosphatase 1alpha; PPP1A; PP-1A
Gene Name PPP1CA
DTT Type
Successful target
[1]
BioChemical Class
Phosphoric monoester hydrolase
UniProt ID
PP1A_HUMAN
TTD ID
T59845
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.1.3.16
Sequence
MSDSEKLNLDSIIGRLLEVQGSRPGKNVQLTENEIRGLCLKSREIFLSQPILLELEAPLK
ICGDIHGQYYDLLRLFEYGGFPPESNYLFLGDYVDRGKQSLETICLLLAYKIKYPENFFL
LRGNHECASINRIYGFYDECKRRYNIKLWKTFTDCFNCLPIAAIVDEKIFCCHGGLSPDL
QSMEQIRRIMRPTDVPDQGLLCDLLWSDPDKDVQGWGENDRGVSFTFGAEVVAKFLHKHD
LDLICRAHQVVEDGYEFFAKRQLVTLFSAPNYCGEFDNAGAMMSVDETLMCSFQILKPAD
KNKGKYGQFSGLNPGGRPITPPRNSAKAKK
Function
Protein phosphatase 1 (PP1) is essential for cell division, and participates in the regulation of glycogen metabolism, muscle contractility and protein synthesis. Involved in regulation of ionic conductances and long-term synaptic plasticity. May play an important role in dephosphorylating substrates such as the postsynaptic density-associated Ca(2+)/calmodulin dependent protein kinase II. Component of the PTW/PP1 phosphatase complex, which plays a role in the control of chromatin structure and cell cycle progression during the transition from mitosis into interphase. Regulates NEK2 function in terms of kinase activity and centrosome number and splitting, both in the presence and absence of radiation-induced DNA damage. Regulator of neural tube and optic fissure closure, and enteric neural crest cell (ENCCs) migration during development. In balance with CSNK1D and CSNK1E, determines the circadian period length, through the regulation of the speed and rhythmicity of PER1 and PER2 phosphorylation. May dephosphorylate CSNK1D and CSNK1E. Dephosphorylates the 'Ser-418' residue of FOXP3 in regulatory T-cells (Treg) from patients with rheumatoid arthritis, thereby inactivating FOXP3 and rendering Treg cells functionally defective. Dephosphorylates CENPA. Dephosphorylates the 'Ser-139' residue of ATG16L1 causing dissociation of ATG12-ATG5-ATG16L1 complex, thereby inhibiting autophagy. Protein phosphatase that associates with over 200 regulatory proteins to form highly specific holoenzymes which dephosphorylate hundreds of biological targets.
KEGG Pathway
mRNA surveillance pathway (hsa03015 )
cGMP-PKG signaling pathway (hsa04022 )
cAMP signaling pathway (hsa04024 )
Oocyte meiosis (hsa04114 )
Cellular senescence (hsa04218 )
Adrenergic signaling in cardiomyocytes (hsa04261 )
Vascular smooth muscle contraction (hsa04270 )
Hippo signaling pathway (hsa04390 )
Focal adhesion (hsa04510 )
Platelet activation (hsa04611 )
Long-term potentiation (hsa04720 )
Dopaminergic synapse (hsa04728 )
Inflammatory mediator regulation of TRP channels (hsa04750 )
Regulation of actin cytoskeleton (hsa04810 )
Insulin signaling pathway (hsa04910 )
Oxytocin signaling pathway (hsa04921 )
Insulin resistance (hsa04931 )
Amphetamine addiction (hsa05031 )
Alcoholism (hsa05034 )
Herpes simplex virus 1 infection (hsa05168 )
Proteoglycans in cancer (hsa05205 )
Diabetic cardiomyopathy (hsa05415 )
Reactome Pathway
DARPP-32 events (R-HSA-180024 )
Downregulation of TGF-beta receptor signaling (R-HSA-2173788 )
Circadian Clock (R-HSA-400253 )
Triglyceride catabolism (R-HSA-163560 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cantharidin DMBP5N3 Molluscum contagiosum infection 1E76 Approved [1]
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5 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CANTHARIDIC_ACID DME32XU Discovery agent N.A. Investigative [1]
MICROCYSTIN-LR DMTMLRN Discovery agent N.A. Investigative [1]
NORCANTHARIDIN DM9B6Y1 Discovery agent N.A. Investigative [2]
PALASONIN DMDTP1R Discovery agent N.A. Investigative [1]
TAUTOMYCIN DMC92DQ Discovery agent N.A. Investigative [1]
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References

1 Serine-threonine protein phosphatase inhibitors: development of potential therapeutic strategies. J Med Chem. 2002 Mar 14;45(6):1151-75.
2 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.