What does EPHA2 stand for?

What does EPHA2 stand for?

EPH receptor A2

What are ephrin ligands?

Ephrin-A ligands are GPI-anchored to the plasma membrane and signal through co-receptors that have not yet been fully defined. Ephrin-B ligands are transmembrane and are linked to an intracellular PDZ-binding motif via a linker containing five tyrosine resides for autophosphorylation.

Is ephrin membrane-bound?

Since ephrin ligands (ephrins) and Eph receptors (Ephs) are both membrane-bound proteins, binding and activation of Eph/ephrin intracellular signaling pathways can only occur via direct cell–cell interaction. …

Are ephrins transcription factors?

In many contexts in which Eph receptor and ephrin signaling has been studied, it is reasonable to assume that they are effectors of morphogenesis expressed downstream of transcription factors that regulate cell identity.

What do integrins do in inflammation?

Integrins regulate cellular growth, proliferation, migration, signaling, and cytokine activation and release and thereby play important roles in cell proliferation and migration, apoptosis, tissue repair, as well as in all processes critical to inflammation, infection, and angiogenesis.

What do integrins do?

How are integrins deactivated?

The mode by which Dok1 competes with talin is regulated by integrin tyrosine phosphorylation. Binding of talin, but not of Dok1, in integrin β tails is reduced by integrin tyrosine phosphorylation [1]. Thus phosphorylation makes integrin inactive.

Where in a cell would you find integrins?

They are expressed exclusively on the surface of white blood cells, where they have an essential role in enabling these cells to fight infection. The β2 integrins mainly mediate cell-cell rather than cell-matrix interactions, binding to specific ligands on another cell, such as an endothelial cell.

How do you activate integrins?

Integrin can be activated from two directions, from the inside by the regulated binding of proteins to the cytoplasmic tails, and from the outside by multivalent ligand binding. In either case, talin binding to the integrin β tails is an essential and the final common step ([10], reviewed in [11]).

What happens when integrins are activated?

Upon ligand binding, integrins activate signal transduction pathways that mediate cellular signals such as regulation of the cell cycle, organization of the intracellular cytoskeleton, and movement of new receptors to the cell membrane.

What are the functions of EphA2 in cancer?

Oncogenic functions and therapeutic targeting of EphA2 in cancer More than 25 years of research and preclinical validation have defined EphA2 receptor tyrosine kinase as a promising molecular target for clinical translation in cancer treatment.

Are there any drugs that can target EphA2?

Molecular, genetic, biochemical, and pharmacological targeting strategies have been extensively tested in vitro and in vivo, and drugs like dasatinib, initially designed to target SRC family kinases, have been found to also target EphA2 activity.

When was EphA2 first detected in human cells?

Its initial detection occurred in 1990 while screening a HeLa cell cDNA library comprising degenerate oligonucleotides engineered to interact with highly conserved domains of tyrosine kinases [ 12 ]. EphA2 was originally termed epithelial cell kinase (eck) since it was detected in most epithelial cells.

What is the role of Eph receptors in cancer?

EphA1, the firstly described Eph receptor, was identified in liver cancer cells while screening for RTKs in 1987 [ 2 ]. Nowadays, there are 14 Eph receptors and 8 related ligands (ephrins) [ 3 ]. Eph receptor signaling contributes to multiple biological events, mostly causing cell-cell repulsion or adhesion.