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

EPHA1 (P21709) - Overview - Molecular Target Synopsis

Protein


EPHA1, Ephrin type-A receptor 1
Enzyme Classification 2.7.10.1
UniProt P21709

Also Known as EPHA1_HUMAN, EPHA1, EPH, EPHT, EPHT1

Receptor tyrosine kinase which binds promiscuously membrane-bound 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. Binds with a low affinity EFNA3 and EFNA4 and with a high affinity to EFNA1 which most probably constitutes its cognate/functional ligand. Upon activation by EFNA1 induces cell attachment to the extracellular matrix inhibiting cell spreading and motility through regulation of ILK and downstream RHOA and RAC. Plays also a role in angiogenesis and regulates cell proliferation. May play a role in apoptosis. Homodimer. Forms a signaling complex with LCK; PTK2B/PYK2 and PI3-kinase upon activation by EFNA1; regulates T-lymphocytes migration. Interacts (via SAM domain) with ILK (via ANK repeats); stimulated by EFNA1 but independent of the kinase activity of EPHA1. Interacts (kinase activity-dependent) with PTK2/FAK1.

3KKA
CO-CRYSTAL STRUCTURE OF THE SAM DOMAINS OF EPHA1 AND EPHA2
RCSB/PDB
Inspect Structure
See all 3D Structures for EPHA1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
976ENSG00000146904ENST00000275815ENSP00000275815P21709-1
490P21709-2
474P21709-3

Drugs


EPHA1 is targeted by Approved Drug Vandetanib. (see details)
Vandetanib

Sub-cellular localization


UniProt: EPHA1 is active in the following subcellular-locations: cell membrane.
GO terms: EPHA1 is active in the following subcellular-locations: integral component of plasma membrane, neuron projection, plasma membrane, receptor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project EPHA1 has gain in 5 cell-lines, loss in 1 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_4, HCC_2998, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NTERA-2, COV413A, LoVo

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, HMEC, H1-hESC

(see details)

RNA Interference


EPHA1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: OAW42, MHM. (see details)

3D Structures


For EPHA1 there are:
4 structures (8 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


EPHA1 has been screened with 364 compounds (592 bioactivities), 15 compounds have bioactivities that show binding affinity of <= 500nM (20 bioactivities). (see details)