Target General Infomation
Target ID
T25464
Former ID
TTDS00363
Target Name
Calcineurin
Gene Name
PPP3CA
Synonyms
Serine/threonine protein phosphatase; PPP3CA
Target Type
Successful
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Kidney diseases; Heart transplantation [ICD9: 996; ICD10: T86]
Organ transplant rejection [ICD9: 279.5, 996; ICD10: D89.8, T86]
Ocular allergy [ICD9: 360-379; ICD10: H00-H59]
Psoriasis [ICD9: 696; ICD10: L40]
Xerophthalmia [ICD10: E50.6-E50.7]
Function
Calcium-dependent, calmodulin-stimulated protein phosphatase. Many of the substrates contain a PxIxIT motif. This subunit may have a role in the calmodulin activation of calcineurin. Dephosphorylates DNM1L, HSPB1 and SSH1.
BioChemical Class
Phosphoric monoester hydrolases
Target Validation
T25464
UniProt ID
EC Number
EC 3.1.3.16
Sequence
MSEPKAIDPKLSTTDRVVKAVPFPPSHRLTAKEVFDNDGKPRVDILKAHLMKEGRLEESV
ALRIITEGASILRQEKNLLDIDAPVTVCGDIHGQFFDLMKLFEVGGSPANTRYLFLGDYV
DRGYFSIECVLYLWALKILYPKTLFLLRGNHECRHLTEYFTFKQECKIKYSERVYDACMD
AFDCLPLAALMNQQFLCVHGGLSPEINTLDDIRKLDRFKEPPAYGPMCDILWSDPLEDFG
NEKTQEHFTHNTVRGCSYFYSYPAVCEFLQHNNLLSILRAHEAQDAGYRMYRKSQTTGFP
SLITIFSAPNYLDVYNNKAAVLKYENNVMNIRQFNCSPHPYWLPNFMDVFTWSLPFVGEK
VTEMLVNVLNICSDDELGSEEDGFDGATAAARKEVIRNKIRAIGKMARVFSVLREESESV
LTLKGLTPTGMLPSGVLSGGKQTLQSATVEAIEADEAIKGFSPQHKITSFEEAKGLDRIN
ERMPPRRDAMPSDANLNSINKALTSETNGTDSNGSNSSNIQ
Drugs and Mode of Action
Drug(s) Cyclosporine Drug Info Approved Psoriasis [536395]
Pimecrolimus Drug Info Approved Atopic dermatitis [536054], [541863]
Tacrolimus Drug Info Approved Organ transplant rejection [537129], [541864]
Tacrolimus Drug Info Phase 3 Ocular allergy [537129], [541864]
Voclosporin Drug Info Phase 3 Psoriasis [537117]
Voclosporin Drug Info Phase 2 Kidney diseases; Heart transplantation [537117]
Cyclosporine Drug Info Investigative Xerophthalmia [536395]
Inhibitor Cyclosporine Drug Info [536395]
L-685,818 Drug Info [534961]
Pimecrolimus Drug Info [537428]
Tacrolimus Drug Info [536119]
Voclosporin Drug Info [537117]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
Calcium signaling pathway
cGMP-PKG signaling pathway
Oocyte meiosis
Apoptosis
Wnt signaling pathway
Axon guidance
VEGF signaling pathway
Osteoclast differentiation
Natural killer cell mediated cytotoxicity
T cell receptor signaling pathway
B cell receptor signaling pathway
Long-term potentiation
Glutamatergic synapse
Dopaminergic synapse
Oxytocin signaling pathway
Glucagon signaling pathway
Alzheimer&#039
s disease
Amyotrophic lateral sclerosis (ALS)
Amphetamine addiction
Tuberculosis
HTLV-I infection
Reactome DARPP-32 events
FCERI mediated Ca+2 mobilization
Ca2+ pathway
WikiPathways Mitochondrial Gene Expression
MAPK Signaling Pathway
G Protein Signaling Pathways
Cardiac Hypertrophic Response
Fc epsilon receptor (FCERI) signaling
Signaling by the B Cell Receptor (BCR)
T-Cell Receptor and Co-stimulatory Signaling
Amyotrophic lateral sclerosis (ALS)
Spinal Cord Injury
Alzheimers Disease
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
Opioid Signalling
MicroRNAs in cardiomyocyte hypertrophy
Physiological and Pathological Hypertrophy of the Heart
References
Ref 536054Emerging drugs for moderate-to-severe psoriasis. Expert Opin Emerg Drugs. 2005 Feb;10(1):35-52.
Ref 536395Cyclosporine and tacrolimus for the treatment of rheumatoid arthritis. Curr Opin Rheumatol. 2007 May;19(3):238-45.
Ref 537117Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
Ref 537129New developments in immunosuppressive therapy for heart transplantation. Expert Opin Emerg Drugs. 2009 Mar;14(1):1-21.
Ref 541863(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6783).
Ref 541864(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6784).
Ref 534961Synergistic antifungal activities of bafilomycin A(1), fluconazole, and the pneumocandin MK-0991/caspofungin acetate (L-743,873) with calcineurin inhibitors FK506 and L-685,818 against Cryptococcus neoformans. Antimicrob Agents Chemother. 2000 Mar;44(3):739-46.
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 536395Cyclosporine and tacrolimus for the treatment of rheumatoid arthritis. Curr Opin Rheumatol. 2007 May;19(3):238-45.
Ref 537117Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
Ref 537428Treatment of chronic blepharokeratoconjunctivitis with local calcineurin inhibitors. Ophthalmologe. 2009 Jul;106(7):635-8.

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