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.
To view external sources of pharmacological information for Eph Receptors, please click here: IUPHAR Receptor CodeView all products for Eph Receptors »
|Gene||Species||Gene Symbol||Gene Accession No.||Protein Accession No.|
|Rat||Efnb1||NM_017089||P52796||View all Eph Receptor Gene Data »|
Literature for Eph Receptors
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Written by Alan Palmer and updated in 2015, this poster summarizes structural and functional changes observed in the progression of Alzheimer's disease (AD), as well as classic AD drug targets. The hypotheses behind the neurobiology of AD are discussed alongside the different stages in disease progression. Compounds available from Tocris are listed.Request copy | Download PDF | View all posters
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