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FKBP prolyl isomerase 1A

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2609

Nomenclature: FKBP prolyl isomerase 1A

Abbreviated Name: FKBP12

Family: Peptidyl-prolyl cis/trans isomerases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 108 20p13 FKBP1A FKBP prolyl isomerase 1A
Mouse - 108 2 G3 Fkbp1a FK506 binding protein 1a
Rat - 108 3q41 Fkbp1a FKBP prolyl isomerase 1A
Previous and Unofficial Names Click here for help
FK506 binding protein 1a | FK506 binding protein 1A | FK506 binding protein 1A, 12kDa | FKBP12 | Peptidyl-prolyl cis-trans isomerase FKBP1A | PKC12 | PPIASE
Database Links Click here for help
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 5.2.1.8

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sirolimus Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.7 pKi 3
pKi 9.7 (Ki 2x10-10 M) [3]
Description: Measuring ability to inhibit the proteins rotamase activity
tacrolimus Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.4 pKi 3
pKi 9.4 (Ki 4x10-10 M) [3]
zotarolimus Small molecule or natural product Primary target of this compound Hs Binding 8.6 pIC50 1
pIC50 8.6 (IC50 2.8x10-9 M) [1]
pimecrolimus Small molecule or natural product Approved drug Primary target of this compound Rn Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 6x10-9 M) [4]
Description: Indirect measurement of primary target inhibition via rotamase inhibition
SLF Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - 6.9 pIC50 2
pIC50 6.9 (IC50 1.14x10-7 M) [2]
Description: Binding affinity determined by a fluorescence polarization assay
View species-specific inhibitor tables
Inhibitor Comments
Further information regarding the mechanism of action and clinical use of pimecrolimus is available in these references:- [5-6].
Immuno Process Associations
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0042098 T cell proliferation IMP
GO:0042110 T cell activation NAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050776 regulation of immune response IMP
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0031398 positive regulation of protein ubiquitination IDA
GO:0042098 T cell proliferation IMP
GO:0042110 T cell activation NAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0019221 cytokine-mediated signaling pathway IMP
GO:1901393 negative regulation of transforming growth factor beta1 activation IDA

References

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1. Garcia-Touchard A, Burke SE, Toner JL, Cromack K, Schwartz RS. (2006) Zotarolimus-eluting stents reduce experimental coronary artery neointimal hyperplasia after 4 weeks. Eur Heart J, 27 (8): 988-93. [PMID:16449248]

2. Gopalakrishnan R, Kozany C, Wang Y, Schneider S, Hoogeland B, Bracher A, Hausch F. (2012) Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52. J Med Chem, 55 (9): 4123-31. [PMID:22455398]

3. Hamilton GS, Steiner JP. (1998) Immunophilins: beyond immunosuppression. J Med Chem, 41 (26): 5119-43. [PMID:9857082]

4. Hultsch T, Müller KD, Meingassner JG, Grassberger M, Schopf RE, Knop J. (1998) Ascomycin macrolactam derivative SDZ ASM 981 inhibits the release of granule-associated mediators and of newly synthesized cytokines in RBL 2H3 mast cells in an immunophilin-dependent manner. Arch Dermatol Res, 290 (9): 501-7. [PMID:9808344]

5. Luger T, Van Leent EJ, Graeber M, Hedgecock S, Thurston M, Kandra A, Berth-Jones J, Bjerke J, Christophers E, Knop J et al.. (2001) SDZ ASM 981: an emerging safe and effective treatment for atopic dermatitis. Br J Dermatol, 144 (4): 788-94. [PMID:11298538]

6. Zuberbier T, Chong SU, Grunow K, Guhl S, Welker P, Grassberger M, Henz BM. (2001) The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils. J Allergy Clin Immunol, 108 (2): 275-80. [PMID:11496246]

Contributors

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How to cite this page

Stephanie Annett, Tracy Robson.
Peptidyl-prolyl cis/trans isomerases: FKBP prolyl isomerase 1A. Last modified on 17/03/2021. Accessed on 16/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2609.