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Updated: Jun 29, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
CXCR4 receptor as a promising target for oncolytic drugs
Yan Lavrovsky1, Yan A Ivanenkov, Konstantin V Balakin
1Small Molecule Drug Discovery, ChemDiv, Inc., San Diego, California 92121, USA.
Abstract:
There has been considerable in vivo evidence that chemokine receptor CXCR4 and its endogenous ligand CXCL12 modulate some important physiological and pathophysiological processes, including cancer metastasis, angiogenesis, invasion, growth and progression. In this review we elucidate key aspects of CXCL12-CXCR4 signaling system with emphasis on peptide-based and small-molecule CXCR4 inhibitors.
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