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Org Biomol Chem. 2012 Aug 14;10(30):5720-31. doi: 10.1039/c2ob25107h. Epub 2012 Apr 19.

Peptide and peptidomimetic ligands for CXC chemokine receptor 4 (CXCR4).

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  • 1Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606-8501, Japan.


The development of novel peptide and peptidomimetic ligands for the CXC chemokine receptor 4 (CXCR4) as therapeutic agents for HIV-1 infection, cancer, and immune system diseases has grown over the last decade. In this perspective article, the design of CXCR4 agonists and antagonists from endogenous stromal cell-derived factor-1 (SDF-1)/CXCL12 and horseshoe crab-derived antimicrobial peptides and their therapeutic and diagnostic applications are described.

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