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Issue 30, 2017
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SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

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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.

Graphical abstract: SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

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Supplementary files

Article information


Submitted
27 Jan 2017
Accepted
16 Mar 2017
First published
17 Mar 2017

Chem. Commun., 2017,53, 4234-4237
Article type
Communication

SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

S. Roy, J. Y. Axup, J. S. Forsyth, R. K. Goswami, B. M. Hutchins, K. M. Bajuri, S. A. Kazane, V. V. Smider, B. H. Felding and S. C. Sinha, Chem. Commun., 2017, 53, 4234
DOI: 10.1039/C7CC00745K

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