Stereoisomeric Peptide Libraries and Peptidomimetics for Designing Selective Inhibitors of the αvβ₃ Integrin for a New Cancer Therapy

Cell–cell and cell–matrix interactions play a major role in biology. An important class of surface receptors are the integrins, which exist in a number of subtypes and are involved in many biological processes, for example embryonic development, blood coagulation, osteoporosis, cancer, and regulation of the balance between proliferation and death (apoptosis) of a cell. Therefore, selective inhibition of specific integrin subtypes is of great pharmaceutical interest. It is possible to develop highly selective and active inhibitors of integrins, especially the α v β 3 subtype, by the novel procedure of spatial screening. The resulting α v β 3 antagonists exhibit activity in the nanomolar range and suppress tumor‐induced angiogenesis (formation of new blood vessels). Tissues with intact blood vessels are not influenced. This opens a promising new way for cancer therapy.