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

EPHA7 (Q15375) - Overview - Molecular Target Synopsis

Protein


EPHA7, Ephrin type-A receptor 7
Enzyme Classification 2.7.10.1
UniProt Q15375

Also Known as EPHA7_HUMAN, EPHA7, EHK3, HEK11

Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A 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. Among GPI-anchored ephrin-A ligands, EFNA5 is a cognate/functional ligand for EPHA7 and their interaction regulates brain development modulating cell-cell adhesion and repulsion. Has a repellent activity on axons and is for instance involved in the guidance of corticothalamic axons and in the proper topographic mapping of retinal axons to the colliculus. May also regulate brain development through a caspase(CASP3)-dependent proapoptotic activity. Forward signaling may result in activation of components of the ERK signaling pathway including MAP2K1, MAP2K2, MAPK1 AND MAPK3 which are phosphorylated upon activation of EPHA7. Heterotetramer upon binding of the ligand. The heterotetramer is composed of an ephrin dimer and a receptor dimer. Oligomerization is probably required to induce biological responses (By similarity). Interacts (via PDZ-binding motif) with GRIP1 and PICK1 (via PDZ domain) (By similarity).

3NRU
LIGAND BINDING DOMAIN OF EPHA7
RCSB/PDB
Inspect Structure
See all 3D Structures for EPHA7

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
998ENSG00000135333ENST00000369303ENSP00000358309Q15375-1
994Q15375-4
993Q15375-2
449Q15375-5
279ENSG00000135333ENST00000369297ENSP00000358303Q15375-3

Drugs


EPHA7 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project EPHA7 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_5, ACHN, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H1581, SNU-398, COV434

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)

RNA Interference


EPHA7 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: DU4475, JIMT1. (see details)

3D Structures


For EPHA7 there are:
4 structures (16 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


EPHA7 has been screened with 484 compounds (796 bioactivities), 15 compounds have bioactivities that show binding affinity of <= 500nM (18 bioactivities). (see details)