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

ERBB3 (P21860) - Overview - Molecular Target Synopsis

Protein


ERBB3, Receptor tyrosine-protein kinase erbB-3
Enzyme Classification 2.7.10.1
UniProt P21860

Also Known as ERBB3_HUMAN, ERBB3, HER3

Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins. Binds to neuregulin-1 (NRG1) and is activated by it; ligand-binding increases phosphorylation on tyrosine residues and promotes its association with the p85 subunit of phosphatidylinositol 3-kinase (PubMed:20682778). May also be activated by CSPG5 (PubMed:15358134). Monomer and homodimer. Heterodimer with each of the other ERBB receptors (Potential). Interacts with CSPG5 (PubMed:15358134). Interacts with GRB7 (PubMed:9516479). Interacts with MUC1 (PubMed:12939402). Interacts with MYOC (By similarity). Interacts with isoform 2 of PA2G4 (PubMed:11325528, PubMed:16832058). Found in a ternary complex with NRG1 and ITGAV:ITGB3 or ITGA6:ITGB4 (PubMed:20682778).

5O4O
HER3 IN COMPLEX WITH FAB MF3178
RCSB/PDB
Inspect Structure
See all 3D Structures for ERBB3

Isoforms / Transcripts (Protein Coding)


Drugs


ERBB3 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


UniProt: ERBB3 is active in the following subcellular-locations: cell membrane, secreted.
GO terms: ERBB3 is active in the following subcellular-locations: apical plasma membrane, basal plasma membrane, basolateral plasma membrane, extracellular space, integral component of plasma membrane, lateral plasma membrane, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ERBB3 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: MALME_3M, SK_MEL_2, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HM7, SK-MEL-2, NCI-H1781

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: MCF-7, HepG2, SK-N-SH

(see details)

RNA Interference


ERBB3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: BEN, MG63. (see details)

3D Structures


For ERBB3 there are:
14 structures (24 chains) solved
13 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

ERBB3 is solved in complex with the approved drug(s):

DB8/BOSUTINIB (4OTW_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ERBB3 has been screened with 1065 compounds (2123 bioactivities), 553 compounds have bioactivities that show binding affinity of <= 500nM (939 bioactivities). (see details)