2. Academic Validation
  3. Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4)

Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4)

  • J Med Chem. 2012 Nov 26;55(22):10287-91. doi: 10.1021/jm300926y.
Jignesh Mungalpara 1,  Stefanie Thiele,  Øystein Eriksen,  Johann Eksteen,  Mette M Rosenkilde,  Jon Våbenø
Affiliations

Affiliation

  • 1 Department of Pharmacy, Faculty of Health Sciences, University of Tromsø, Breivika, NO-9037 Tromsø, Norway.
PMID: 23043442 DOI: 10.1021/jm300926y
Abstract

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.

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