The chemical diversity and structure-based evolution of non-peptide CXCR4 antagonists with diverse therapeutic potential.
作者： Dian Peng , Bin Cao , Ying-Jun Zhou , Ya-Qiu Long
DOI: 10.1016/J.EJMECH.2018.02.043
关键词:
摘要: Abstract The CXC chemokine receptor 4 (CXCR4) is a highly reserved G-protein coupled 7-transmembrane (TM) which consists of 352 amino acids. CXCR4 has only one endogenous ligand CXCL12, besides several other natural nonchemokine ligands such as extracellular ubiquitin and noncognate MIF. strongly binds to CXCL12 the resulting CXCLl2/CXCR4 axis molecular basis their various biological functions, include: (1) mediating immune inflammatory response; (2) regulation hematopoietic stem cell migration homing; (3) an essential co-receptor for HIV entry into host cells; (4) participation in process embryonic development; (5) malignant tumor invasion metastasis; (6) myocardial infarction, ischemic stroke acute kidney injury. Correspondingly, antagonists find potential therapeutic applications infection, well migration, inflammation, immune-related diseases, diseases. Recently, great achievements have been made number non-peptide with diversity scaffolds discovered. In this review, discovery small molecule focused on structures, activities, evolution development representative comprehensively described. central role diverse cellular signaling pathways its involvement diseases progressions are discussed well.
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