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 ?
WHIM syndrome is a primary genetic immunodeficiency disease caused by mutations in the CXCR4 receptor gene resulting susceptibility to certain infections.
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.
The study showed that administration of autologous bone marrow derived cells expressing the CXCR4 receptor, five to ten days after an AMI, significantly reduces the cumulative incidence of major adverse clinical cardiac events, including death, heart failure and recurrent cardiac ischemia.
13] using a mouse model have found that the chemokine CXCL12, highly expressed in tissues prone to breast cancer metastasis, can trigger chemotaxis of malignant mammary cells in vitro through interaction with the CXCR4 receptor present at high levels in breast cancer cells.
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.
In the present study, we investigated the CXCR4 receptor expression in splenocytes and thymocytes of protein restricted mice infected with Listeria monocytogenes.
CAFs are capable of secreting elevated levels of stromal cell-derived factor 1 (SDF-1), also called CXCL12, which plays a central role in the promotion of tumour growth and angiogenesis; CAF-derived SDF-1 not only stimulates carcinoma growth directly through the CXCR4 receptor expressed on tumour cells, but also serves to recruit endothelial progenitor cells into tumours [11,12].
The CXCR4 receptor specifically recognizes the chemokine stromal derived factor 1 (SDF-I), which acts as a potent chemoattractant for stem cells and assists in retaining stem cells within the bone marrow environment.
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.