Target Information
| Target General Information | Top | |||||
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| Target ID |
T40491
(Former ID: TTDI00641)
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| Target Name |
Serine/threonine PP2A-alpha (PPP2CA)
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| Synonyms |
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform; Replication protein C; RP-C; PP2A-alpha
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| Gene Name |
PPP2CA
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Molluscum contagiosum [ICD-11: 1E76] | |||||
| Function |
PP2A can modulate the activity of phosphorylase B kinase casein kinase 2, mitogen-stimulated S6 kinase, and MAP-2 kinase. Cooperates with SGO2 to protect centromeric cohesin from separase-mediated cleavage in oocytes specifically during meiosis I. Can dephosphorylate SV40 large T antigen and p53/TP53. Activates RAF1 by dephosphorylating it at 'Ser-259'. PP2A is the major phosphatase for microtubule-associated proteins (MAPs).
Click to Show/Hide
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| BioChemical Class |
Phosphoric monoester hydrolase
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| UniProt ID | ||||||
| EC Number |
EC 3.1.3.16
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| Sequence |
MDEKVFTKELDQWIEQLNECKQLSESQVKSLCEKAKEILTKESNVQEVRCPVTVCGDVHG
QFHDLMELFRIGGKSPDTNYLFMGDYVDRGYYSVETVTLLVALKVRYRERITILRGNHES RQITQVYGFYDECLRKYGNANVWKYFTDLFDYLPLTALVDGQIFCLHGGLSPSIDTLDHI RALDRLQEVPHEGPMCDLLWSDPDDRGGWGISPRGAGYTFGQDISETFNHANGLTLVSRA HQLVMEGYNWCHDRNVVTIFSAPNYCYRCGNQAAIMELDDTLKYSFLQFDPAPRRGEPHV TRRTPDYFL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | VP-102 | Drug Info | Phase 3 | Molluscum contagiosum infection | [2] | |
| 2 | LB-100 | Drug Info | Phase 2 | Astrocytoma | [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 2 Inhibitor drugs | + | ||||
| 1 | VP-102 | Drug Info | [1] | |||
| 2 | LB-100 | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| References | Top | |||||
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| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | ClinicalTrials.gov (NCT03377803) Cantharidin Application in Molluscum Patients (CAMP-2). U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT03027388) Protein Phosphatase 2A Inhibitor, in Recurrent Glioblastoma. U.S. National Institutes of Health. | |||||
| REF 4 | Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72. | |||||
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