EPH receptor A2 (ephrin type-A receptor 2) is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...
that in humans is encoded by the ''EPHA2''
gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
.
Function
This gene belongs to the
ephrin receptor
Eph receptors (Ephs, after erythropoietin-producing human hepatocellular receptors) are a group of receptor (biochemistry), receptors that are activated in response to binding with Ephrin, Eph receptor-interacting proteins (Ephrins). Ephs form th ...
subfamily of the
protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the
nervous system
In biology, the nervous system is the complex system, highly complex part of an animal that coordinates its behavior, actions and sense, sensory information by transmitting action potential, signals to and from different parts of its body. Th ...
. Receptors in the EPH subfamily typically have a single
kinase domain and an extracellular region containing a
Cys-rich domain and 2
fibronectin type III repeats. The ephrin receptors are divided into two groups based on the similarity of their extracellular domain sequences and their affinities for binding
ephrin-A and ephrin-B ligands. This gene encodes a protein that binds ephrin-A ligands.
Clinical significance
It may be implicated in
BRAF mutated
melanoma
Melanoma is the most dangerous type of skin cancer; it develops from the melanin-producing cells known as melanocytes. It typically occurs in the skin, but may rarely occur in the mouth, intestines, or eye (uveal melanoma). In very rare case ...
s becoming resistant to BRAF-inhibitors and
MEK inhibitor
A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase enzymes MEK1 and/or MEK2.
They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers. (See MAPK/ERK pathway#Clinical signifi ...
s. It is also the receptor by which
Kaposi's sarcoma-associated herpesvirus
Kaposi's sarcoma-associated herpesvirus (KSHV) is the ninth known human herpesvirus. It is also called Human herpesvirus 8, or HHV-8 in short. This virus causes Kaposi's sarcoma, a cancer commonly occurring in AIDS patients, as well as primary ...
(KSHV) enters host cells;
small molecule
In molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; ...
inhibitors of EphA2 have shown some ability to block KSHV entry into human cells.
Interactions
EPH receptor A2 has been shown to
interact with:
*
Ephrin A1
*
ACP1
Low molecular weight phosphotyrosine protein phosphatase is an enzyme that in humans is encoded by the ''ACP1'' gene.
The product of this gene belongs to the phosphotyrosine protein phosphatase family of proteins. It functions as an acid phosphata ...
*
Grb2
Growth factor receptor-bound protein 2, also known as Grb2, is an adaptor protein involved in signal transduction/ cell communication. In humans, the GRB2 protein is encoded by the ''GRB2'' gene.
The protein encoded by this gene binds recepto ...
,
*
PIK3R1
Phosphatidylinositol 3-kinase regulatory subunit alpha is an enzyme that in humans is encoded by the ''PIK3R1'' gene.
Function
Phosphatidylinositol 3-kinase phosphorylates the inositol ring of phosphatidylinositol at the 3-prime position. ...
,
and
*
SHC1
SHC-transforming protein 1 is a protein that in humans is encoded by the ''SHC1'' gene. SHC has been found to be important in the regulation of apoptosis and drug resistance in mammalian cells.
SCOP
A ( or ) was a poet as represented in Old ...
.
[
It was also shown that ]doxazosin
Doxazosin, sold under the brand name Cardura among others, is a medication used to treat symptoms of benign prostatic hyperplasia (enlarged prostate), hypertension (high blood pressure), and post-traumatic stress disorder (PTSD). For high bloo ...
is a small molecule agonist of EPH receptor A2.
See also
* Vasculogenic mimicry
References
Further reading
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External links
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Tyrosine kinase receptors
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