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Review
. 2015;7(10):1261-83.
doi: 10.4155/fmc.15.64.

Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists

Jon Våbenø  1 , Bengt Erik Haug  2 , Mette M Rosenkilde  3
Affiliations
Review

Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists

Jon Våbenø et al. Future Med Chem. 2015.

Abstract

Over the last 5 years, X-ray structures of CXCR4 in complex with three different ligands (the small-molecule antagonist IT1t, the polypeptide antagonist CVX15 and the viral chemokine antagonist vMIP-II) have been released. In addition to the inherent scientific value of these specific X-ray structures, they provide a reliable structural foundation for studies of the molecular interactions between CXCR4 and its key peptide ligands (CXCL12 and HIV-1 gp120), and serve as valuable templates for further development of small-molecule CXCR4 antagonists with therapeutic potential. We here review recent computational studies of the molecular interactions between CXCR4 and its peptide ligands - based on the X-ray structures of CXCR4 - and the current status of small-molecule peptide and peptidomimetic CXCR4 antagonists.

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