Target Information
Target General Infomation | |||||
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Target ID |
T76059
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Former ID |
TTDC00307
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Target Name |
FK506-binding protein 1A
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Gene Name |
FKBP1A
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Synonyms |
12 kDa FKBP; FK-binding protein 12; FKBP-12; Immunophilin FKBP12; Immunophillin FKBP; PPIase; Peptidyl-prolyl cis-trans isomerase; Rotamase; FKBP1A
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Target Type |
Successful
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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.
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BioChemical Class |
Cis-trans-isomerases
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Target Validation |
T76059
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UniProt ID | |||||
EC Number |
EC 5.2.1.8
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Sequence |
MGVQVETISPGDGRTFPKRGQTCVVHYTGMLEDGKKFDSSRDRNKPFKFMLGKQEVIRGW
EEGVAQMSVGQRAKLTISPDYAYGATGHPGIIPPHATLVFDVELLKLE |
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Structure |
1A7X; 1B6C; 1BKF; 1BL4; 1D6O; 1D7H; 1D7I; 1D7J
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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 524154 | ClinicalTrials.gov (NCT01744223) Safety Study of Gene Modified Donor T-cells Following Partially Mismatched Stem Cell Transplant. U.S. National Institutes of Health. | ||||
Ref 534115 | Clearing of psoriasis by a novel immunosuppressive macrolide. J Invest Dermatol. 1996 Apr;106(4):701-10. | ||||
Ref 545206 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002452) | ||||
Ref 534115 | Clearing of psoriasis by a novel immunosuppressive macrolide. J Invest Dermatol. 1996 Apr;106(4):701-10. | ||||
Ref 534700 | Redesigning 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 536923 | Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. |
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