Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4)
Research output: Contribution to journal › Journal article › peer-review
In the absence of an experimentally determined binding mode for the cyclopentapeptide CXCR4 antagonists, we have rationally designed conformationally constrained analogues to further probe the small peptide binding pocket of CXCR4. Two different rigidification strategies were employed, both resulting in highly potent ligands (9 and 13). The information provided by this cyclopentapeptide ligand series will be very valuable in the development of novel peptidomimetic CXCR4 antagonists.
|Journal||Journal of Medicinal Chemistry|
|Number of pages||5|
|Publication status||Published - 9 Oct 2012|
- Drug Design, Humans, Ligands, Models, Molecular, Molecular Conformation, Peptides, Cyclic, Peptidomimetics, Protein Conformation, Receptors, CXCR4