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
  • 1. Department of Cell and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. [email protected].
PMID: 28357420 DOI: 10.1039/c7cc00745k
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.

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