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Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4)

Zachariassen, Zack Georg; Thiele, Stefanie; Berg, Erik; Rasmussen, Pernille; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik
Journal article
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URI
https://hdl.handle.net/1956/12518
Date
2014
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  • Department of Chemistry [251]
Original version
https://doi.org/10.1016/j.bmc.2014.07.004
Abstract
Structure–activity relationship studies of the cyclopentapeptide CXCR4 antagonists (cyclo(-l-/d-Arg1-Arg2-2-Nal3-Gly4-d-Tyr5-)) suggest that the l-/d-Arg1-Arg2-2-Nal3 tripeptide sequence contained within these cyclopentapeptides serves as a recognition motif for peptidic CXCR4 antagonists. Starting by dissecting the cyclopentapeptide structure and reintroducing cyclic constraints in a stepwise manner, we here report a novel class of scaffold-based tripeptidomimetic CXCR4 antagonists based on the d-Arg-Arg-2-Nal motif. Biological testing of the prototype compounds showed that they represent new peptidomimetic hits; importantly, the modular nature of the scaffold provides an interesting starting point for future ligand optimization.
Publisher
Elsevier
Copyright
Copyright 2014 The Authors

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