BL‐8040 CXCR4 antagonist is safe and demonstrates antileukemic activity in combination with cytarabine for the treatment of relapsed/refractory acute myelogenous leukemia: An open‐label safety and efficacy phase 2a study
Sign Up to like & getrecommendations! Published in 2020 at "Cancer"
DOI: 10.1002/cncr.33338
Abstract: CXCR4 mediates the retention and survival of acute myelogenous leukemia blasts in bone marrow and contributes to their resistance to chemotherapy. The authors evaluated a combination of the high‐affinity CXCR4 antagonist BL‐8040 with high‐dose cytarabine… read more here.
Keywords: relapsed refractory; cxcr4 antagonist; myelogenous leukemia; phase study ... See more keywords
Dimerization of the Peptide CXCR4-Antagonist on Macromolecular and Supramolecular Protraction Arms Affords Increased Potency and Enhanced Plasma Stability.
Sign Up to like & getrecommendations! Published in 2022 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.2c00034
Abstract: Peptides are prime drug candidates due to their high specificity of action but are disadvantaged by low proteolytic stability. Here, we focus on the development of stabilized analogues of EPI-X4, an endogenous peptide antagonist of… read more here.
Keywords: cxcr4 antagonist; antagonist macromolecular; dimerization peptide; stability ... See more keywords
Abstract 2270: Combination of CXCR4 antagonist and anti-PD1 therapy results in significant mobilization and increased infiltration of myeloid cells into the metastatic liver microenvironment of PDAC
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-2270
Abstract: Pancreatic adenocarcinoma (PDAC) is extremely lethal and resistant to checkpoint immunotherapy, characterized by an immunosuppressive tumor microenvironment consisting of stromal and myeloid cells. Prior studies have demonstrated the utility of targeting the chemokine signaling axis… read more here.
Keywords: cxcr4 antagonist; increased infiltration; myeloid cells; myeloid ... See more keywords
Evaluation of pharmacodynamic (PD) biomarkers in patients with metastatic pancreatic cancer treated with BL-8040, a novel CXCR4 antagonist.
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DOI: 10.1200/jco.2018.36.5_suppl.88
Abstract: 88Background: BL-8040 is a novel CXCR4 antagonist being developed for multiple oncology indications. Preclinical studies demonstrated that BL-8040 increases the number of immune cells in peripheral blood and promotes CD8+ T cell infiltration into orthotropic… read more here.
Keywords: cxcr4 antagonist; metastatic pancreatic; 8040 novel; patients metastatic ... See more keywords
Shang-Ke-Huang-Shui and coptisine alleviate osteoarthritis in the knee of monosodium iodoacetate-induced rats through inhibiting CXCR4 signaling.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of ethnopharmacology"
DOI: 10.2139/ssrn.4237126
Abstract: ETHNOPHARMACOLOGICAL RELEVANCE Shang-Ke-Huang-Shui (SKHS) is a classic traditional Chinese medicine formula originally from the southern China city of Foshan. It has been widely used in the treatment of osteoarthritis (OA) but underlying molecular mechanisms remain… read more here.
Keywords: cxcr4 signaling; cxcr4 antagonist; cartilage; cxcr4 ... See more keywords
CXCR4 antagonist AMD3100 elicits analgesic effect and restores the GlyRα3 expression against neuropathic pain
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Pain Research"
DOI: 10.2147/jpr.s139619
Abstract: Objective Chemokine CXCL12 and its receptor CXCR4 have been reported to play a critical role in neurogenesis and neuronal differentiation. Recently, some reports have implicated this chemokine signaling in the pathogenesis of many kinds of… read more here.
Keywords: antagonist amd3100; cxcr4 antagonist; expression; neuropathic pain ... See more keywords
A Novel CXCR4 Antagonist CX549 Induces Neuroprotection in Stroke Brain
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DOI: 10.3727/096368916x693563
Abstract: C-X-C chemokine receptor type 4 (CXCR4) is a receptor for a pleiotropic chemokine CXCL12. Previous studies have shown that the acute administration of the CXCR4 antagonist AMD3100 reduced neuroinflammation in stroke brain and mobilized bone… read more here.
Keywords: cx549; cxcr4 antagonist; stroke brain; novel cxcr4 ... See more keywords