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

EPHA6 (Q9UF33) - Overview - Molecular Target Synopsis

Protein


EPHA6, Ephrin type-A receptor 6
Enzyme Classification 2.7.10.1
UniProt Q9UF33

Also Known as EPHA6_HUMAN, EPHA6, EHK2, HEK12

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. 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 ANKS1A (via SAM domain).

Isoforms / Transcripts (Protein Coding)


Drugs


EPHA6 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


UniProt: EPHA6 is active in the following subcellular-locations: membrane.
GO terms: EPHA6 is active in the following subcellular-locations: integral component of plasma membrane, neuron projection, nucleoplasm, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project EPHA6 has gain in 3 cell-lines, loss in 1 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, HS578T, KM12

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: KMS-27, SNU-398, L-363

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


EPHA6 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: PL5, SCC47. (see details)

3D Structures


At greater than 75% identity similarity to EPHA6 there are:
1 structures (1 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


EPHA6 has been screened with 133 compounds (195 bioactivities), 19 compounds have bioactivities that show binding affinity of <= 500nM (33 bioactivities). (see details)