FKBP prolyl isomerase 1A | 5.2.-.- Cis-trans-isomerases | IUPHAR/BPS Guide to PHARMACOLOGY

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FKBP prolyl isomerase 1A

Target not currently curated in GtoImmuPdb

Target id: 2609

Nomenclature: FKBP prolyl isomerase 1A

Family: 5.2.-.- Cis-trans-isomerases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
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
FK506 binding protein 1a | FK506 binding protein 1A | FK506 binding protein 1A, 12kDa | FKBP12 | Peptidyl-prolyl cis-trans isomerase FKBP1A | PKC12 | PPIASE
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sirolimus Hs Inhibition 9.7 pKi 2
pKi 9.7 (Ki 2x10-10 M) [2]
Description: Measuring ability to inhibit the proteins rotamase activity
tacrolimus Hs Inhibition 9.4 pKi 2
pKi 9.4 (Ki 4x10-10 M) [2]
zotarolimus Hs Binding 8.6 pIC50 1
pIC50 8.6 (IC50 2.8x10-9 M) [1]
pimecrolimus Rn Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6x10-9 M) [3]
Description: Indirect measurement of primary target inhibition via rotamase inhibition
View species-specific inhibitor tables
Inhibitor Comments
Further information regarding the mechanism of action and clinical use of pimecrolimus is available in these references:- [4-5].
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 1 GO processes
GO:0019221 cytokine-mediated signaling pathway IMP


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

3. 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]

4. 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]

5. 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]

How to cite this page

5.2.-.- Cis-trans-isomerases: FKBP prolyl isomerase 1A. Last modified on 27/03/2019. Accessed on 03/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,