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Keywords:

  • conformation analysis;
  • diketopiperazines;
  • molecular modeling;
  • peptides;
  • peptidomimetics
Thumbnail image of graphical abstract

Cyclo-[DKP-RGD] peptidomimetics obtained by cyclization of bifunctional diketopiperazines (DKP) with RGD, inhibit vitronectin binding to integrins αvβ3 and αvβ5 at low nanomolar concentration. Conformational studies (NMR spectroscopy and calculations) reveal that the highest affinity ligands display an extended RGD arrangement, in which the carboxylate and guanidinium groups act like an electrostatic clamp, interacting with charged regions of the receptor binding site. For more details see the Full Paper by C. Gennari et al. on page 6195 ff.