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FKBP prolyl isomerase 4

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Target id: 3176

Nomenclature: FKBP prolyl isomerase 4

Abbreviated Name: FKBP52

Family: Peptidyl-prolyl cis/trans isomerases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 459 12p13.33 FKBP4 FKBP prolyl isomerase 4
Mouse - 458 6 F3 Fkbp4 FK506 binding protein 4
Rat - 458 4q42 Fkbp4 FKBP prolyl isomerase 4
Previous and Unofficial Names Click here for help
FKBP52 | FKBP-52
Database Links Click here for help
Alphafold Q02790 (Hs), P30416 (Mm), Q9QVC8 (Rn)
BRENDA 5.2.1.8
ChEMBL Target CHEMBL4050 (Hs)
Ensembl Gene ENSG00000004478 (Hs), ENSMUSG00000030357 (Mm), ENSRNOG00000006444 (Rn)
Entrez Gene 2288 (Hs), 14228 (Mm), 260321 (Rn)
Human Protein Atlas ENSG00000004478 (Hs)
KEGG Enzyme 5.2.1.8
KEGG Gene hsa:2288 (Hs), mmu:14228 (Mm), rno:260321 (Rn)
OMIM 600611 (Hs)
Pharos Q02790 (Hs)
RefSeq Nucleotide NM_002014 (Hs), NM_010219 (Mm), NM_001191863 (Rn)
RefSeq Protein NP_002005 (Hs), NP_034349 (Mm), NP_001178792 (Rn)
UniProtKB Q02790 (Hs), P30416 (Mm), Q9QVC8 (Rn)
Wikipedia FKBP4 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure Analysis of FKBP52, Complex with I63
PDB Id:  4LAY
Ligand:  SLF
Resolution:  1.7Å
Species:  Human
References:  1
Enzyme Reaction Click here for help
EC Number: 5.2.1.8

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 19b [PMID: 37058391] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.1 pKi 3
⤷ pKi 6.1 (Ki 7.74x10-7 M) [3]
SLF Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - 5.0 pIC50 2
⤷ pIC50 5.0 (IC50 9.37x10-6 M) [2]
Description: Binding affinity determined by a fluorescence polarization assay

References

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1. Bracher A, Kozany C, Hähle A, Wild P, Zacharias M, Hausch F. (2013) Crystal structures of the free and ligand-bound FK1-FK2 domain segment of FKBP52 reveal a flexible inter-domain hinge. J Mol Biol, 425 (22): 4134-44. [PMID:23933011]

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. Knaup FH, Meyners C, Sugiarto WO, Wedel S, Springer M, Walz C, Geiger TM, Schmidt M, Sisignano M, Hausch F. (2023) Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51. J Med Chem, 66 (8): 5965-5980. [PMID:37058391]

Contributors

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