Eph Receptors

Eph receptors are the largest family of receptor tyrosine kinases (RTKs) and are divided into two subclasses, EphA and EphB. Originally identified as mediators of axon guidance, Eph receptors are implicated in many processes, particularly cancer development and progression.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5290 KYL
EphA4 kinase inhibitor; neuroprotective
4405 NVP BHG 712
Potent EphB4 kinase inhibitor

Eph (or ephrin) receptors are the largest family of receptor tyrosine kinases (RTKs) and are divided into two subclasses, EphA and EphB, based on sequence homology and binding affinities. The receptors are widely expressed and are involved in the control of cell positioning, tissue patterning, organ patterning and cell survival.

Both receptor and ligand are membrane bound, so that interaction between the two occurs at sites of cell-cell contact, and uniquely, initiates a bidirectional signaling cascade. Receptor activation results in the clustering, followed by tyrosine phosphorylation and signaling of the receptors (referred to as forward signaling), while simultaneously triggering a response in the ligand-bearing cells (known as reverse signaling). The ligands for EphA receptors are glycosyl phosphatidylinositol (GPI)-linked and cell-surface bound, whereas EphB receptor ligands are transmembrane.

The Eph-ephrin signaling response is highly complex and the outcome is dependent on context in that it can differ according to cell, tissue and organ type, with the result that the same Eph-ephrin interaction can result in diametrically opposed responses, such as tumor promotion or suppression, in different tissues. Activation of the Eph receptor leads to changes in the actin cytoskeleton and cell-cell or cell-substrate adhesion, as well as cell motility, survival and proliferation. Activated Ephs also interact with major cytosolic signaling pathways and may activate or inhibit MAPK, PI 3-K or Wnt pathways. They can also modulate or be modulated by growth factor receptors, including VEGFR, FGFR or EGFR.

Eph receptors were originally identified as mediators in axon path finding, but are also implicated in bone morphogenesis and homeostasis, immunological and inflammatory responses, angiogenesis, stem cell plasticity, learning and memory and Alzheimer's disease. They are of particular interest in the study of the mechanisms of tumor growth and progression, as well as nerve injury and regeneration.

External sources of pharmacological information for Eph Receptors :

    Literature for Eph Receptors

    Cancer

    Cancer Research Product Guide

    A collection of over 750 products for cancer research, the guide includes research tools for the study of:

    • Cancer Metabolism
    • Epigenetics in Cancer
    • Receptor Signaling
    • Cell Cycle and DNA Damage Repair
    • Angiogenesis
    • Invasion and Metastasis
    Kinases

    Kinases Product Listing

    A collection of over 400 products for kinase research, the listing includes inhibitors of:

    • Receptor Tyrosine Kinases
    • Protein Kinases A, C, D and G
    • PI-3 Kinase, Akt and mTOR
    • MAPK Signaling
    • Receptor Serine/Threonine Kinases
    Neurodegeneration

    Neurodegeneration Product Guide

    A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

    • Alzheimer's disease
    • Parkinson's disease
    • Huntington's disease
    Alzheimer's

    Alzheimer's Poster

    Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.

    Eph Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    EFNA1 Human EFNA1 NM_004428 P20827
    Mouse Efna1 NM_010107 P52793
    Rat Efna1 NM_053599 P97553
    EFNA2 Human EFNA2 NM_001405 O43921
    Mouse Efna2 NM_007909 P52801
    Rat Efna2 NM_001168670 NP_001162141
    EFNA3 Human EFNA3 NM_004952 P52797
    Mouse Efna3 NM_010108 O08545
    Rat Efna3 XM_001072657 XP_001072657
    EFNA4 Human EFNA4 NM_005227 P52798
    Mouse Efna4 NM_007910 Q3UQB5
    Rat Efna4 NM_001107692 NP_001101162
    EFNA5 Human EFNA5 NM_001962 P52803
    Mouse Efna5 NM_207654 O08543
    Rat Efna5 NM_053903 P97605
    EFNB1 Human EFNB1 NM_004429 P98172
    Mouse Efnb1 NM_010110 P52795
    Rat Efnb1 NM_017089 P52796
    EFNB2 Human EFNB2 NM_004093 P52799
    Mouse Efnb2 NM_010111 P52800
    Rat Efnb2 NM_001107328 NP_001100798
    EFNB3 Human EFNB3 NM_001406 Q15768
    Mouse Efnb3 NM_007911 Q543Q7
    Rat Efnb3 NM_001100980 ABQ23904