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Integrin aVb3 (CD51/CD61)

In vitro studies have identified selective integrin aVb3 antagonists that could be useful for treating cancer. Synthesis of arginine-glycine-aspartic (RGD) acid peptidomimetics based on a b-homotyrosine scaffold yielded integrin aVb3 antagonists with EC50 values in the low nanomolar or subnanomolar range and good selectivity for integrin aVb3 over integrin a5b1. Next steps could include comparing the RGD acid peptidomimetics with Merck KGaA's cilengitide in animal models.
Cilengitide is a cyclic peptide angiogenesis inhibitor that potently blocks integrin aVb3 but also has activity against the related integrin a5b1, which prevents selective targeting. The molecule is in Phase II testing to treat head and neck cancer and lung cancer.
At least five other companies have integrin aVb3-targeting compounds in Phase II testing or earlier to treat various cancers.

SciBX 7(17); doi:10.1038/scibx.2014.484
Published online May 1, 2014

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Neubauer, S. et al. J. Med. Chem.; published online March 23, 2014;
Contact: Horst Kessler, Technical University Munich, Munich, Germany