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SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth
Saumya Roy1, Jun Y Axup, Jane S Forsyth
1Department of Cell and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. ssinha@rockefeller.edu.
Chemical Communications (Cambridge, England)
|March 31, 2017
Abstract:
Cell-targeting conjugates of Saporin 6, a ribosome inactivating protein (RIP), were prepared using the Saporin Ala 157 Cys mutant, a small molecule inhibitor (SMI) of integrins αvβ3/αvβ5, and a potent cytotoxin, auristatin F (AF). The conjugates selectively and potently inhibited proliferation of tumor cells expressing the target integrins. We anticipate that the small molecule-RIP bioconjugate approach can be broadly applied using other small molecule drugs.