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

FES (P07332) - Overview - Molecular Target Synopsis

Protein


FES, Tyrosine-protein kinase Fes/Fps
Enzyme Classification 2.7.10.2
UniProt P07332

Also Known as FES_HUMAN, FES, FPS

Tyrosine-protein kinase that acts downstream of cell surface receptors and plays a role in the regulation of the actin cytoskeleton, microtubule assembly, cell attachment and cell spreading. Plays a role in FCER1 (high affinity immunoglobulin epsilon receptor)-mediated signaling in mast cells. Acts down-stream of the activated FCER1 receptor and the mast/stem cell growth factor receptor KIT. Plays a role in the regulation of mast cell degranulation. Plays a role in the regulation of cell differentiation and promotes neurite outgrowth in response to NGF signaling. Plays a role in cell scattering and cell migration in response to HGF-induced activation of EZR. Phosphorylates BCR and down-regulates BCR kinase activity. Phosphorylates HCLS1/HS1, PECAM1, STAT3 and TRIM28. Homooligomer. Interacts with BCR. Interacts (when activated, via coiled coil domain) with TRIM28. Interacts (via SH2 domain) with phosphorylated EZR, MS4A2/FCER1B and HCLS1/HS1. Interacts with phosphorylated KIT. Interacts with FLT3. Interacts (via F-BAR domain) with soluble tubulin. Interacts (via SH2 domain) with microtubules.

4E93
CRYSTAL STRUCTURE OF HUMAN FELINE SARCOMA VIRAL ONCOGENE HOMOLOGUE (V- FES)IN COMPLEX WITH TAE684
RCSB/PDB
Inspect Structure
See all 3D Structures for FES

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FES is active in the following subcellular-locations: cell junction, cell membrane, cytoplasm, cytoplasmic vesicle, cytoskeleton, cytosol, focal adhesion, golgi apparatus.
GO terms: FES is active in the following subcellular-locations: cytoplasm, cytoplasmic vesicle, cytosol, extrinsic component of cytoplasmic side of plasma membrane, focal adhesion, Golgi apparatus, microtubule cytoskeleton.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FES has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, UACC_257, MOLT_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: THP-1, ML-2, HEL

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: HUVEC, CD14-positive monocyte, CD34-positive mobilized cell

(see details)

RNA Interference


FES was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, CAOV3. (see details)

3D Structures


For FES there are:
8 structures (8 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


FES has been screened with 827 compounds (1433 bioactivities), 14 compounds have bioactivities that show binding affinity of <= 500nM (19 bioactivities). (see details)