CXCR4 antagonist
Mobilization of hematopoietic stem cells with the novel CXCR4 antagonist POL6326 (balixafortide) in healthy volunteers—results of a dose escalation trial
... peptidic CXCR4 antagonist POL5551, a close analogue of the clinical stage compound balixafortide (POL6326), shows a very wide pharmacodynamic range in preclinical mod- els and at optimal doses even ...
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Inhibitory Mechanism of the CXCR4 Antagonist T22 against Human Immunodeficiency Virus Type 1 Infection
... downregulating CXCR4 surface expression. Inhibition of anti-CXCR4 MAb (R6-48 and 12G5) binding by T22 suggested that the peptide interacts with the N terminus and two ECLs of CXCR4 ...to CXCR4 ...
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<p>The CXCR4 Antagonist, AMD3100, Reverses Mesenchymal Stem Cell-Mediated Drug Resistance in Relapsed/Refractory Acute Lymphoblastic Leukemia</p>
... molecule CXCR4 antagonist AMD3100 (plerixafor) could mobilize AML cells from the protective BM microenvironment by blocking CXCL12 binding to CXCR4, resulting in susceptibility to ...surface ...
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CXCR4 antagonist AMD3100 elicits analgesic effect and restores the GlyRα3 expression against neuropathic pain
... of CXCR4 in the ipsilateral SC after SNL were studied at baseline on Day 14 and Day ...rats), CXCR4 antagonist AMD3100 was used to assess the effects against ...
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The CXCR4 antagonist plerixafor enhances the effect of rituximab in diffuse large B-cell lymphoma cell lines
... (CXCR4) antagonist plerixafor (AMD3100) in a related type of lymphoma (Burkitt lymphoma) [10, ...This CXCR4 antagonist displays a low-risk safety profile and has already been approved by the ...
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Plerixafor (a CXCR4 antagonist) following myeloablative allogeneic hematopoietic stem cell transplantation enhances hematopoietic recovery
... reversible CXCR4 antagonist) after allogeneic HSCT to enhance hematopoietic cell recovery in patients re- ceiving myeloablative allogeneic ...to CXCR4 blockade, we previously found that ...
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Inhibition of Human Immunodeficiency Virus Replication by a Dual CCR5/CXCR4 Antagonist
... 6), CXCR4 and CCR5 are the two most relevant coreceptors for HIV entry (14, ...fore, CXCR4 antagonists may be useful in delaying the onset of ...and CXCR4 may be highly valuable for inhibiting viral ...
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Distinct Molecular Pathways to X4 Tropism for a V3-Truncated Human Immunodeficiency Virus Type 1 Lead to Differential Coreceptor Interactions and Sensitivity to a CXCR4 Antagonist
... for CXCR4 usage (7, 21, 43, 50, 59, 60, 63, ...whether CXCR4 utilization could be regained on a back- ground in which this critical V3-ECL interaction had been ablated and, if so, by what ...in CXCR4 ...
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The brain-penetrating CXCR4 antagonist, PRX177561, increases the antitumor effects of bevacizumab and sunitinib in preclinical models of human glioblastoma
... novel CXCR4 antagonist showing good brain penetration was demonstrated to reduce growth in vitro and in vivo of GBM cells and induce glioma stem cell differentiation ...the CXCR4 and ...since ...
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The CXCR4 antagonist plerixafor (AMD3100) promotes proliferation of Ewing sarcoma cell lines in vitro and activates receptor tyrosine kinase signaling
... to CXCR4 receptor expressions of our cell line ...affect CXCR4 sur- face expression and function [27, 29]. Because such CXCR4 splicing variants have been reported in Ewing sarcoma [30, 31], we first ...
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T134, a Small-Molecule CXCR4 Inhibitor, Has No Cross-Drug Resistance with AMD3100, a CXCR4 Antagonist with a Different Structure
... T22, an analog of polyphemusin II (18 amino acid residues), was found to block T-tropic human immuno- deficiency virus type 1 (HIV-1) entry into target cells as a CXCR4 inhibitor. We synthesized T134, a small ...
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Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia
... IgG1 CXCR4 antagonist antibody, induced cell death of patient-derived primary CLL-B cells, in presence or absence of stromal ...on CXCR4 expression, required antibody bivalency, involved reactive ...
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Co-delivery of sorafenib and metapristone encapsulated by CXCR4-targeted PLGA-PEG nanoparticles overcomes hepatocellular carcinoma resistance to sorafenib
... Combining sorafenib with other chemotherapeutics has demonstrated to enhance anti-tumor efficacy and re- lieve acquired resistance to sorafenib, which provides a promising therapeutic strategy for treatment of HCC [34 – ...
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Cancer-associated fibroblasts promote the progression of endometrial cancer via the SDF-1/CXCR4 axis
... (CXCR4) antagonist) was used to block the SDF-1/CXCR4 ...and CXCR4 expressions were analyzed in xenotransplanted tumors and 348 cases by ...and CXCR4 expression upregulation accompanied ...
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Identification of CXCR4 Domains That Support Coreceptor and Chemokine Receptor Functions
... expressing CXCR4 or mutant ...pressing CXCR4 was observed only in the presence of sCD4, consistent with the conformational changes induced by CD4 that are believed to expose the chemokine receptor binding ...
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Targeting CXCR4 potentiates anti-PD-1 efficacy modifying the tumor microenvironment and inhibiting neoplastic PD-1
... powerful CXCR4 antagonist Pep R54 [20] in a xeno- graft model of human ...for CXCR4 antagonism targeting tumoral cells and ...and CXCR4. In athymic mice, double targeting of CXCR4 and ...
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Nef M1, a CXCR4 Peptide Antagonist, Enhances Apoptosis and Inhibits Primary Tumor Growth and Metastasis in Breast Cancer
... of CXCR4 was deter- mined by ...human CXCR4 primers used for PCR were: a) hCXCR4-1, 1097 bp of CXCR4 (forward): 5’-atgaaacttggggcgaggac-3’; (reverse): 5’-cggtgtagttatctgaagtg-3’; b) hCXCR4-2, 922 bp ...
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Co-expression of Lgr5 and CXCR4 characterizes cancer stem-like cells of colorectal cancer
... control, CXCR4+/Lgr5-, Lgr5+/CXCR4- or Lgr5+/CXCR4+ cells were transplanted ...Lgr5+/ CXCR4+ cells was significantly greater than tumor mass from the other cell populations (Figure ...
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Expression of Chemokine Receptor CXCR4 in Primary and Metastatic Neuroblastoma Expression of CXCR4 in Neuroblastoma
... marrow. CXCR4 expression was compared with International Neuroblastoma Staging System (INSS) stages of ...of CXCR4 expression and clinical stages (P ≤ 0.05). CXCR4 expression was found to be highly ...
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Vol 70, No 1 (2018)
... plicated in cell death [83]. In contrast to Ca v channels, CXCL12α has no influence on the transcription rate of Trpm2 after 30 min of incubation, in contrast to overnight incubation, which caused a lowering of the ...
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