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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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Publication details

The article was received on 27 Jan 2017, accepted on 16 Mar 2017 and first published on 17 Mar 2017


Article type: Communication
DOI: 10.1039/C7CC00745K
Citation: Chem. Commun., 2017,53, 4234-4237
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    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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