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

EPHB2 (P29323) - Overview - Molecular Target Synopsis

Protein


EPHB2, Ephrin type-B receptor 2
Enzyme Classification 2.7.10.1
UniProt P29323

Also Known as EPHB2_HUMAN, EPHB2, DRT, EPHT3, EPTH3, ERK, HEK5, TYRO5

Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Functions in axon guidance during development. Involved in the guidance of commissural axons, that form a major interhemispheric connection between the 2 temporal lobes of the cerebral cortex. Also involved in guidance of contralateral inner ear efferent growth cones at the midline and of retinal ganglion cell axons to the optic disk. In addition to axon guidance, also regulates dendritic spines development and maturation and stimulates the formation of excitatory synapses. Upon activation by EFNB1, abolishes the ARHGEF15-mediated negative regulation on excitatory synapse formation. Controls other aspects of development including angiogenesis, palate development and in inner ear development through regulation of endolymph production. Forward and reverse signaling through the EFNB2/EPHB2 complex regulate movement and adhesion of cells that tubularize the urethra and septate the cloaca. May function as a tumor suppressor. Heterotetramer upon binding of the ligand (By similarity). The heterotetramer is composed of an ephrin dimer and a receptor dimer (PubMed:17897949). Interacts (via PDZ-binding motif) with GRIP1 and PICK1 (via PDZ domain) (By similarity). Interacts with ARHGEF15; mediates ARHGEF15 phosphorylation, ubiquitination and degradation by the proteasome (By similarity). Interacts with AQP1; involved in endolymph production in the inner ear (By similarity). Interacts with SPSB1 and SPSB4 (PubMed:28931592). The phosphorylated form interacts with RASA1 (via SH2 domain 1) (By similarity). Interacts with EFNA5.

3ZFM
CRYSTAL STRUCTURE OF EPHB2
RCSB/PDB
Inspect Structure
See all 3D Structures for EPHB2

Isoforms / Transcripts (Protein Coding)


Drugs


EPHB2 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project EPHB2 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: COLO205, UO_31, SF_295

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: COLO 205, COLO 206F, SW 1463

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: IMR-90, HUVEC, SK-N-SH_RA

(see details)

RNA Interference


EPHB2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MIAPACA2, BT20. (see details)

3D Structures


For EPHB2 there are:
4 structures (12 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


EPHB2 has been screened with 777 compounds (1412 bioactivities), 18 compounds have bioactivities that show binding affinity of <= 500nM (26 bioactivities). (see details)