Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

FKBP4 (Q02790) - Overview - Molecular Target Synopsis

Protein


FKBP4, Peptidyl-prolyl cis-trans isomerase FKBP4
Enzyme Classification 5.2.1.8
UniProt Q02790

Also Known as FKBP4_HUMAN, FKBP4, FKBP52

Immunophilin protein with PPIase and co-chaperone activities. Component of steroid receptors heterocomplexes through interaction with heat-shock protein 90 (HSP90). May play a role in the intracellular trafficking of heterooligomeric forms of steroid hormone receptors between cytoplasm and nuclear compartments. The isomerase activity controls neuronal growth cones via regulation of TRPC1 channel opening. Acts also as a regulator of microtubule dynamics by inhibiting MAPT/TAU ability to promote microtubule assembly. May have a protective role against oxidative stress in mitochondria. Homodimer (By similarity). Interacts with GLMN (PubMed:12604780). Associates with HSP90AA1 and HSP70 in steroid hormone receptor complexes. Also interacts with peroxisomal phytanoyl-CoA alpha-hydroxylase (PHYH). Interacts with NR3C1 and dynein. Interacts with HSF1 in the HSP90 complex. Associates with tubulin. Interacts with MAPT/TAU (By similarity). Interacts (via TPR domain) with S100A1, S100A2 and S100A6; the interaction is Ca(2+) dependent. Interaction with S100A1 and S100A2 (but not with S100A6) leads to inhibition of FKBP4-HSP90 interaction. Interacts with dynein; causes partially NR3C1 transport to the nucleus.

4TW8
THE FK1-FK2 DOMAINS OF FKBP52 IN COMPLEX WITH IFIT-FL
RCSB/PDB
Inspect Structure
See all 3D Structures for FKBP4

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FKBP4 is active in the following subcellular-locations: axon, cell projection, cytoplasm, cytoskeleton, cytosol, mitochondrion, nucleus.
GO terms: FKBP4 is active in the following subcellular-locations: axonal growth cone, cytoplasm, cytosol, extracellular exosome, microtubule, mitochondrion, neuronal cell body, nucleoplasm, perinuclear region of cytoplasm, protein-containing complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FKBP4 has gain in 5 cell-lines, loss in 1 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, T47D, OVCAR_8

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MDA-MB-134-VI, NTERA-2, T-47D

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, A549, HMEC

(see details)

3D Structures


For FKBP4 there are:
10 structures (18 chains) solved
4 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

FKBP4 is solved in complex with the approved drug(s):

RAP/SIROLIMUS (4DRJ_A),
FK5/TACROLIMUS (4LAX_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


FKBP4 has been screened with 125 compounds (165 bioactivities), 2 compounds have bioactivities that show binding affinity of <= 500nM (2 bioactivities). (see details)