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  2. SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

  • Chem Commun (Camb). 2017 Apr 11;53(30):4234-4237. doi: 10.1039/c7cc00745k.
Saumya Roy 1 Jun Y Axup Jane S Forsyth Rajib K Goswami Benjamin M Hutchins Krishna M Bajuri Stephanie A Kazane Vaughn V Smider Brunhilde H Felding Subhash C Sinha
Affiliations

Affiliation

  • 1 Department of Cell and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. ssinha@rockefeller.edu.
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 αvβ3vβ5, 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.

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