FK506 binding protein 1A

Target id: 2609

Nomenclature: FK506 binding protein 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

   GtoImmuPdb view: OFF :     Currently no data for FK506 binding protein 1A in GtoImmuPdb

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

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units 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].

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. 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: FK506 binding protein 1A. Last modified on 29/01/2016. Accessed on 22/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2609.