Target Information

Target General Infomation
Target ID
T76059
Former ID
TTDC00307
Target Name
FK506-binding protein 1A
Gene Name
FKBP1A
Synonyms
12 kDa FKBP; FK-binding protein 12; FKBP-12; Immunophilin FKBP12; Immunophillin FKBP; PPIase; Peptidyl-prolyl cis-trans isomerase; Rotamase; FKBP1A
Target Type
Successful
Disease Coronary artery restenosis; Multiple myeloma [ICD9:203; ICD10: I51.89, C90]
Parkinson's disease [ICD9: 332; ICD10: G20]
Pruritus [ICD9: 698; ICD10: L29]
Transplant rejection [ICD9: 279.5, 996; ICD10: D89.8, T86]
Function
May play a role in modulation of ryanodine receptor isoform-1 (RYR-1), a component of the calcium release channel of skeletal muscle sarcoplasmic reticulum. There are four molecules of FKBP12 per skeletal muscle RYR.
BioChemical Class
Cis-trans-isomerases
Target Validation
T76059
UniProt ID
P62942
EC Number
EC 5.2.1.8
Sequence
MGVQVETISPGDGRTFPKRGQTCVVHYTGMLEDGKKFDSSRDRNKPFKFMLGKQEVIRGW
EEGVAQMSVGQRAKLTISPDYAYGATGHPGIIPPHATLVFDVELLKLE
Structure
1A7X; 1B6C; 1BKF; 1BL4; 1D6O; 1D7H; 1D7I; 1D7J
Drugs and Mode of Action
Drug(s) Rapamycin Drug Info Approved Coronary artery restenosis; Multiple myeloma [545206], [551871]
GPI-1485 Drug Info Phase 2 Parkinson's disease [536266]
SDZ-281-240 Drug Info Phase 2 Pruritus [534115]
AP1903 Drug Info Phase 1/2 Transplant rejection [524154]
Gpi-1046 Drug Info Terminated Parkinson's disease [546468]
Inhibitor 4-Hydroxy-2-Butanone Drug Info [551393]
FKB-001 Drug Info [551393]
Gpi-1046 Drug Info [551374]
Heptyl-Beta-D-Glucopyranoside Drug Info [551391]
L-709,587 Drug Info [551393]
Methyl Methylsulfinylmethyl Sulfide Drug Info [551393]
MYRISTIC ACID Drug Info [551374]
Rapamycin Immunosuppressant Drug Drug Info [551393]
Modulator AP1903 Drug Info [529386], [534700]
SDZ-281-240 Drug Info [534115]
Binder GPI-1485 Drug Info [536923]
Rapamycin Drug Info [538069]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
Ref 524154ClinicalTrials.gov (NCT01744223) Safety Study of Gene Modified Donor T-cells Following Partially Mismatched Stem Cell Transplant. U.S. National Institutes of Health.
Ref 534115Clearing of psoriasis by a novel immunosuppressive macrolide. J Invest Dermatol. 1996 Apr;106(4):701-10.
Ref 536266Emerging drugs for Parkinson's disease. Expert Opin Emerg Drugs. 2006 Sep;11(3):403-17.
Ref 545206Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002452)
Ref 546468Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008349)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 529386Using gene transfer to circumvent off-target effects. Gene Ther. 2008 May;15(10):759-64.
Ref 534115Clearing of psoriasis by a novel immunosuppressive macrolide. J Invest Dermatol. 1996 Apr;106(4):701-10.
Ref 534700Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.
Ref 536923Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
Ref 538069Neural roles of immunophilins and their ligands. Mol Neurobiol. 1997 Oct;15(2):223-39.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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