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

Roland Haubner, Dirk Finsinger, Horst Kessler

Research output: Contribution to journalArticlepeer-review

408 Scopus citations

Abstract

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 αvβ3 subtype, by the novel procedure of spatial screening. The resulting αvβ3 antagonists exhibit activity in the nanomolar range and sup-press 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.

Original languageEnglish
Pages (from-to)1374-1389
Number of pages16
JournalAngewandte Chemie International Edition in English
Volume36
Issue number13-14
DOIs
StatePublished - 1997

Keywords

  • Cyclic peptides
  • Integrins
  • Receptors
  • Structure-activity relationships

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