Top ▲

peptidylprolyl isomerase A

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2751

Nomenclature: peptidylprolyl isomerase A

Family: 5.2.-.- Cis-trans-isomerases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 165 7p13 PPIA peptidylprolyl isomerase A
Mouse - 164 11 3.97 cM Ppia peptidylprolyl isomerase A
Rat - 164 14q21 Ppia peptidylprolyl isomerase A
Previous and Unofficial Names Click here for help
CYPA | peptidylprolyl isomerase A (cyclophilin A)
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Complex of human peptidyl-prolyl cis-trans isomerase A (PPIA, cyclophilin A) and cyclosporin A
PDB Id:  2X2C
Ligand:  cyclosporin A
Resolution:  2.41Å
Species:  Human
References:  2
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
cyclosporin A Peptide Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 1
pIC50 8.3 (IC50 5x10-9 M) Inhibition of the phosphatase activity of calcineurin in Jurkat cells. [1]
Inhibitor Comments
Cyclosporin A does not inhibit calcineurin activity directly. It must be in complex with its immunophilin 'receptor', cyclophilin A (PPIA), before it is able to bind and inhibit calcineurin [3].
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 1 GO processes
GO:0019064 fusion of virus membrane with host plasma membrane TAS
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0043312 neutrophil degranulation TAS
GO:0050900 leukocyte migration TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0035722 interleukin-12-mediated signaling pathway TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS

References

Show »

1. Fruman DA, Klee CB, Bierer BE, Burakoff SJ. (1992) Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc. Natl. Acad. Sci. U.S.A., 89 (9): 3686-90. [PMID:1373887]

2. Lammers M, Neumann H, Chin JW, James LC. (2010) Acetylation regulates cyclophilin A catalysis, immunosuppression and HIV isomerization. Nat. Chem. Biol., 6 (5): 331-7. [PMID:20364129]

3. Liu J, Farmer Jr JD, Lane WS, Friedman J, Weissman I, Schreiber SL. (1991) Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell, 66 (4): 807-15. [PMID:1715244]

How to cite this page

5.2.-.- Cis-trans-isomerases: peptidylprolyl isomerase A. Last modified on 29/01/2016. Accessed on 02/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2751.