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

GRB14 (Q14449) - Overview - Molecular Target Synopsis

Protein


GRB14, Growth factor receptor-bound protein 14
UniProt Q14449

Also Known as GRB14_HUMAN, GRB14

Adapter protein which modulates coupling of cell surface receptor kinases with specific signaling pathways. Binds to, and suppresses signals from, the activated insulin receptor (INSR). Potent inhibitor of insulin-stimulated MAPK3 phosphorylation. Plays a critical role regulating PDPK1 membrane translocation in response to insulin stimulation and serves as an adapter protein to recruit PDPK1 to activated insulin receptor, thus promoting PKB/AKT1 phosphorylation and transduction of the insulin signal. Interacts with the cytoplasmic domain of the autophosphorylated insulin receptor (INSR), through the SH2 domain (By similarity). Interacts with GRB14 (via BPS domain); this interaction protects the tyrosines in the activation loop on INSR from dephosphorylation. Binds to the ankyrin repeat region of TNKS2 via its N-terminus. Interacts with activated NRAS. Interacts (via SH2 domain) with TEK/TIE2 (tyrosine phosphorylated).

4K81
CRYSTAL STRUCTURE OF THE GRB14 RA AND PH DOMAINS IN COMPLEX WITH GTP- LOADED H-RAS
RCSB/PDB
Inspect Structure
See all 3D Structures for GRB14

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: GRB14 is active in the following subcellular-locations: cytoplasm, endosome membrane.
GO terms: GRB14 is active in the following subcellular-locations: cytoplasm, cytosol, endosome membrane, intracellular membrane-bounded organelle, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GRB14 has gain in 1 cell-lines, loss in 3 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, TK_10, OVCAR_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G84, HCC1500, HCC1319

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, NHLF, HSMM

(see details)

3D Structures


For GRB14 there are:
3 structures (7 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GRB14 has been screened with compounds ( bioactivities). (see details)