Selection of a CXCR4 antagonist from a human heavy chain CDR3-derived phage library (pages 2867–2878)
Andy Chevigné, Aurélie Fischer, Julie Mathu, Manuel Counson, Nadia Beaupain, Jean-Marc Plesséria, Jean-Claude Schmit and Sabrina Deroo
Version of Record online: 27 JUN 2011 | DOI: 10.1111/j.1742-4658.2011.08208.x
In contrast to negative selection campaigns with random peptide libraries on a peptide corresponding to the second extracellular loop of CXCR4, a single campaign with a human heavy chain CDR3 library resulted in one CXCR4 antagonist (IC50 = 23 μM). Strength and efficacy of the HCDR3 libraries reside in the combination of multiple size peptides and naturally biased sequence variation.