CXCR4

(redirected from CXCR4 receptor)

CXCR4

A gene on chromosome 2q21 that encodes a seven-transmembrane G protein-coupled receptor belonging to the CXC chemokine receptor family, which binds specifically to stromal cell-derived factor-1, transducing a signal by increasing intracellular calcium ions and enhancing MAPK1/MAPK3 activation. It acts as a receptor for extracellular ubiquitin, is involved in haematopoiesis and in cardiac ventricular septum formation, plays a role in gastrointestinal tract vascularisation by regulating vascular branching and/or remodelling in endothelial cells, may be involved in cerebellar development and, in the CNS, may mediate hippocampal-neuron survival.

Molecular pathology
CXCR4 acts with the CD4 to support HIV entry into cells; it is highly expressed in breast cancer cells. CXCR4 mutations cause WHIM (warts, hypogammaglobulinaemia, infections, and myelokathexis) syndrome.
References in periodicals archive ?
In contrast, we found no difference in CXCR4 receptor expression in HeLa cells treated with LPS at any time point investigated (Fig.
However, little is known whether these compounds act directly as antagonist of CXCR4 receptor and its signaling pathways.
In addition, expression of the CXCR4 receptor in FLT3 mutated AML is also correlated with poor outcomes.
While the other chemokines bind to forms of HIV that use either the CCR5 or the CXCR4 receptor, CXCL4 can bind to and block infection by a wide variety of HIV strains, no matter what their receptor specificity.
Upon binding of SDF-1 to its CXCR4 receptor, CXCR4 undergoes dimerization and activates downstream signal transduction pathways through heterotrimeric G-protein activation.
The patent entitled "Therapeutic Chemokine Receptor Antagonists", with a term lasting to March 2019, covers therapeutics compositions comprising CXCR4 receptor antagonists and builds on a patent granted earlier this year which focused on methods of use of the same compounds.
But the beta Chemokines only block some HIV viruses, those that use the CCR5 receptor on the CD4 cell to enter the cell--not viruses that use the CXCR4 receptor, which often evolve later in HIV infection.
In contrast, the link between WHIM syndrome and the CXCR4 receptor suggests that any drugs targeting this chemokine receptor could have significant side effects, cautions Diaz.
Research Reported in PNAS Demonstrates Allosteric Activation of CXCR4 Receptor to Mobilize Bone Marrow Hematopoietic Stem Cells -
To date, the T4-L method has been successfully applied to solve at least nine novelGPCR structures, including the beta 2 adrenergic receptor, the D3 dopamine receptor, the CXCR4 receptor, the H1 histamine receptor, the S1P1 receptor and the A2A adenosine receptor, which have been reported in Science and Nature.
As the CXCR4 receptor has been shown to be strongly associated with multiple cancer cell types, we are eager to test this potential therapeutic in advanced or metastatic solid tumor cancer patients.
The T4-L method has been validated and successfully applied to solve at least thirteen novel GPCR structures, including the beta 2 adrenergic receptor, the D3 dopamine receptor, the CXCR4 receptor, the H1 histamine receptor, the S1P1 receptor, the A2A adenosine receptor, the mu, delta, and kappa-opioid receptors, the M2 and M3 muscarinic receptors which have been reported in Science and Nature.