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CXCR4 Theranostics: A Potential Game Changer in Solid Tumors and Hematological Malignancies
An overexpression of CXCR4 receptors is reported in at least 30 different human solid tumors and hematological malignancies. This overexpression is... -
Case Study #5: CXCR4-Targeted Radiotherapeutics
Radiopharmaceutical therapy (RPT) has become a mainstay of modern oncology but remains limited to solid tumors, including orphan diseases such as... -
Targeting CXCR4/CXCL12 axis via [177Lu]Lu-DOTAGA.(SA.FAPi)2 with CXCR4 antagonist in triple-negative breast cancer
PurposeRadiopharmaceutical therapies targeting fibroblast activation protein (FAP) have shown promising efficacy against many tumor types. But...
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Structural basis of dimerization of chemokine receptors CCR5 and CXCR4
G protein-coupled receptors (GPCRs) are prominent drug targets responsible for extracellular-to-intracellular signal transduction. GPCRs can form...
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Interplay between androgen and CXCR4 chemokine signaling in myelin repair
In men, reduced levels of testosterone are associated with the prevalence and progression of multiple sclerosis (MS), a chronic and disabling...
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CXCR4 overexpression in chronic lymphocytic leukemia associates with poorer prognosis: A prospective, single-center, observational study
Controversial data have been reported on the prognostic value of C-X-C motif chemokine receptor 4 (CXCR4) in chronic lymphocytic leukemia (CLL). This...
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CXCL12–CXCR4 Axis in Cancer Metastasis
The malignancy that leads to the most fatalities is characterized by metastasis. Due to continually develo** research in the biology of cancer as... -
LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration
BackgroundG protein-coupled receptor heteromerization is believed to exert dynamic regulatory impact on signal transduction. CXC chemokine receptor 4...
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Glucocorticoids paradoxically promote steroid resistance in B cell acute lymphoblastic leukemia through CXCR4/PLC signaling
Glucocorticoid (GC) resistance in childhood relapsed B-cell acute lymphoblastic leukemia (B-ALL) represents an important challenge. Despite decades...
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Targeting CXCR4 impaired T regulatory function through PTEN in renal cancer patients
BackgroundTregs trafficking is controlled by CXCR4. In Renal Cell Carcinoma (RCC), the effect of the new CXCR4 antagonist, R54, was explored in...
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Influence of corticosteroid treatment on CXCR4 expression in DLBCL
BackgroundCXCR4-targeted radioligand therapy (RLT) with [ 177 Lu]Lu/[ 90 Y]Y-PentixaTher has recently evolved as a promising therapeutic option for...
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CXC chemokine receptor 4 (CXCR4) blockade in cancer treatment
CXC chemokine receptor type 4 (CXCR4) is a member of the G protein-coupled receptors (GPCRs) superfamily and is specific for CXC chemokine ligand 12...
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WHIM Syndrome-linked CXCR4 mutations drive osteoporosis
WHIM Syndrome is a rare immunodeficiency caused by gain-of-function CXCR4 mutations. Here we report a decrease in bone mineral density in 25% of WHIM...
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CREB1-driven CXCR4hi neutrophils promote skin inflammation in mouse models and human patients
Neutrophils have a pathogenic function in inflammation via releasing pro-inflammatory mediators or neutrophil extracellular traps (NETs). However,...
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Notch3-regulated microRNAs impair CXCR4-dependent maturation of thymocytes allowing maintenance and progression of T-ALL
Malignant transformation of T-cell progenitors causes T-cell acute lymphoblastic leukemia (T-ALL), an aggressive childhood lymphoproliferative...
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Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system
Chemokine receptors constitute an important subfamily of G protein-coupled receptors (GPCRs), and they are critically involved in a broad range of...
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Demethylation in promoter region of severely damaged hepatocytes enhances chemokine receptor CXCR4 gene expression
The liver is known to possess remarkable regenerative potential, but persistent inflammation or severe acute injury can lead to liver fibrosis and...
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Caulis Spatholobi extracts inhibit osteosarcoma growth and metastasis through suppression of CXCR4/PI3K/AKT signaling
BackgroundThe therapeutic potential of Caulis Spatholobi (CS) extracts against various cancers has been well documented, yet its impact and mechanism...
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The importance of CXCR4 expression in tumor stroma as a potential biomarker in pancreatic cancer
BackgroundPancreatic ductal adenocarcinoma (PDAC) is one of the main causes of cancer mortality in the world. A characteristic feature of this cancer...