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

EPHA5 (P54756) - Overview - Molecular Target Synopsis

Protein


EPHA5, Ephrin type-A receptor 5
Enzyme Classification 2.7.10.1
UniProt P54756

Also Known as EPHA5_HUMAN, EPHA5, BSK, EHK1, HEK7, TYRO4

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 most probably constitutes the cognate/functional ligand for EPHA5. Functions as an axon guidance molecule during development and may be involved in the development of the retinotectal, entorhino-hippocampal and hippocamposeptal pathways. Together with EFNA5 plays also a role in synaptic plasticity in adult brain through regulation of synaptogenesis. In addition to its function in the nervous system, the interaction of EPHA5 with EFNA5 mediates communication between pancreatic islet cells to regulate glucose-stimulated insulin secretion. 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 SAM domain) with SAMD5 (via SAM domain).

4ET7
CRYSTAL STRUCTURE OF EPH RECEPTOR 5
RCSB/PDB
Inspect Structure
See all 3D Structures for EPHA5

Isoforms / Transcripts (Protein Coding)


Drugs


EPHA5 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


UniProt: EPHA5 is active in the following subcellular-locations: axon, cell membrane, cell projection, dendrite.
GO terms: EPHA5 is active in the following subcellular-locations: axon, dendrite, external side of plasma membrane, integral component of plasma membrane, neuron projection, neuronal cell body, perinuclear region of cytoplasm, plasma membrane, receptor complex, rough endoplasmic reticulum.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project EPHA5 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: NCI_H522, NCI_H460, SNB_75

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: COV434, NCI-H522, MG-63

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


EPHA5 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MCF12A, TE10. (see details)

3D Structures


For EPHA5 there are:
2 structures (2 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


EPHA5 has been screened with 327 compounds (571 bioactivities), 12 compounds have bioactivities that show binding affinity of <= 500nM (19 bioactivities). (see details)