Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 22, Pages 10287-10291Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm300926y
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Funding
- Research Council of Norway [190728/V30]
- University of Copenhagen
- Danish Medical Research Council
- Medical Research Council [G9818340B] Funding Source: researchfish
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In the absence of an experimentally determined binding made 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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