Introduction of CXCR4
CXCR4 is a G protein-coupled receptor in the CXC chemokine receptor family, encoded by CXCR4 gene. It is one of seven CXC chemokine receptors (CXCR1-CXCR7) in mammals. The receptors can recognize CXC chemokine that possesses an E-L-R amino acid motif. CXCR4 is widely expressed in many human tissues, such as lymph node, bone marrow. Recently, most studies focus on the role of CXCR4 in the pathological process of cancer.
|Basic Information of CXCR4|
|Protein Name||C-X-C chemokine receptor type 4|
FB22, HM89, LAP3, LCR1, NPYR, WHIM, CD184, LAP-3, LESTR,
NPY3R, NPYRL, WHIMS, HSY3RR, NPYY3R, D2S201E
|Organism||Homo sapiens (Human)|
Function of CXCR4 Membrane Protein
CXCR4 binds to its ligands, C-X-C chemokine CXCL12/SDF-1, leading to the activation of G protein-dependent signaling pathways. It is involved in a number of biological processes, such as organogenesis, hematopoiesis, and immune response. The previous studies showed that CXCR4 plays an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Besides, CXCR4 also plays a key role in the progression of cancer through activating several signal pathways, such as SAPK/JNK, MAPK, and ERK1/2. These pathways mediate tumor cells proliferation, survival, and migration. And the expression of CXCR4 has been detected highly in 23 different cancers of various origins while low or scantily in many healthy tissues. Low expression of CXCR4 can decrease cell growth, promote cell apoptosis. Additionally, CXCR4 acts as a coreceptor for HIV-1 regulating HIV infection.
Fig.1 Signal Transduction Pathways and Regulation of CXCR4. (Busillo, 2007)
Application of CXCR4 Membrane Protein in Literature
The in vitro study shows that CXCR4 antagonist plerixafor can increase Ewing sarcoma cells viability and proliferation and promote cells chemotactic migration toward to plerixafor. And proliferative plerixafor responses are involved in the activation of multiple receptor tyrosine kinases. A multi-kinase inhibitor of both PDGFRB and the CXCR4 downstream kinase SRC can reduce this activation in some cell lines. These suggest that PDGFRB can act as a potential therapeutic co-target for CXCR4 in Ewing sarcoma.
The study identifies that CXCR4-directed radioligand therapy (in combination with additional radioligand therapy) is feasible before allogeneic stem cell transplantation in diffuse large B cell lymphoma.
The finding shows that chemokine receptors may play an essential role in the progression of head and neck squamous cell carcinoma as well as the metastasis and recurrence of the regional lymph node. Low CXCR4 levels are significantly associated with both disease-specific and disease-free survival.
The study indicates that the high CXCR4 levels are observed in pulmonary arterial hypertension groups compared to controls, suggesting that CXCR4 associated with the pathogenesis of pulmonary arterial hypertension. Besides stem cells may play an important role in pulmonary vascular remodeling.
The study shows that silencing the CXCR4 gene with shRNA in SW626 ovarian cancer cells can increased apoptosis signal-regulating kinase 1 (ASK1) mRNA expression and phosphorylated-c-Jun protein expression, decrease extracellular-signal-regulated kinase (ERK1/2) protein expression, with a significance. At all, silencing the CXCR4 gene with shRNA can reduce cell proliferation, promote cell apoptosis, possibly regulated by MAPK signaling pathway.
CXCR4 Preparation Options
To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-CXCR4 antibody development services.
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