Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T25464 Target Info
Target Name Calcineurin (PPP3CA)
Synonyms
Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform; Calmodulin-dependent calcineurin A subunit alpha isoform; CNA; CAM-PRP catalytic subunit; CALNA
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Target Type Successful Target
Gene Name PPP3CA
Biochemical Class Phosphoric monoester hydrolase
UniProt ID
PP2BA_HUMAN
Co-Targets of This Target  Top
Co-Target Name FK506-binding protein 1A (FKBP1A) Successful Target
UniProt ID FKB1A_HUMAN
Gene Name FKBP1A
Synonyms
Rotamase; Peptidyl-prolyl cis-trans isomerase FKBP1A; PPIase FKBP1A; Immunophillin FKBP; Immunophilin FKBP12; FKBP12; FKBP1; FKBP-1A; FKBP-12; FK-binding protein 12; Calstabin-1; 12 kDa FKBP; 12 kDa FK506-binding protein
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Representative Drug(s) Tacrolimus Drug Info Ki = 0.4 nM [1]
Co-Target Name Serine/threonine-protein kinase mTOR (mTOR) Successful Target
UniProt ID MTOR_HUMAN
Gene Name MTOR
Synonyms
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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Representative Drug(s) Tacrolimus Drug Info IC50 = 0.95 nM [2]
Co-Target Name Cytochrome P450 3A (CYP3A) Successful Target
UniProt ID CP3A4_HUMAN; CP3A5_HUMAN; CP3A7_HUMAN; CP343_HUMAN
Gene Name NO-GeName
Representative Drug(s) Tacrolimus Drug Info Ki = 360 nM [3]
Co-Target Name Albendazole monooxygenase (CYP3A4) Clinical trial Target
UniProt ID CP3A4_HUMAN
Gene Name CYP3A4
Synonyms
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) Tacrolimus Drug Info IC50 = 120 nM [3]
Co-Target Name FK506-binding protein 5 (FKBP5) Literature-reported Target
UniProt ID FKBP5_HUMAN
Gene Name FKBP5
Synonyms
Peptidyl-prolyl cis-trans isomerase FKBP5; PPIase FKBP5; HSP90-binding immunophilin; FKBP54; FKBP51; FKBP-51; FKBP-5; FF1 antigen; Androgen-regulated protein 6; AIG6; 54 kDa progesterone receptor-associated immunophilin; 51 kDa FKBP; 51 kDa FK506-binding protein
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Representative Drug(s) Tacrolimus Drug Info Ki = 79 nM [4]
Co-Target Name Splicing factor 3B subunit 3 (SF3B3) Co-Target
UniProt ID SF3B3_HUMAN
Gene Name SF3B3
Synonyms
SAP 130; Pre-mRNA-splicing factor SF3b 130 kDa subunit; SF3b130; STAF130; Spliceosome-associated protein 130
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Representative Drug(s) Tacrolimus Drug Info IC50 = 10.9 nM [5]
Co-Target Name Cytochrome P450 3A5 (CYP3A5) Co-Target
UniProt ID CP3A5_HUMAN
Gene Name CYP3A5
Synonyms
Cytochrome P450-PCN3; CYPIIIA5
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Representative Drug(s) Tacrolimus Drug Info IC50 = 140 nM [3]
References  Top
REF 1 Immunophilins: beyond immunosuppression. J Med Chem. 1998 Dec 17;41(26):5119-43.
REF 2 A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma. J Med Chem. 2004 Sep 23;47(20):4950-7.
REF 3 Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro. Drug Metab Dispos. 2012 Apr;40(4):655-61.
REF 4 Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51. J Med Chem. 2016 Mar 24;59(6):2410-22.
REF 5 Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nat Chem Biol. 2007 Sep;3(9):570-5.

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