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SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

Roy, Saumya, Axup, Jun Y., Forsyth, Jane S., GoswamiCurrent address: Department of Organic Chemistry, Indian Association for the Cultivation of Science, Jadavpur, Kolkata, India., Rajib K., Hutchins, Benjamin M., Bajuri, Krishna M., KazaneCurrent address: Center for Therapeutic Innovation (CTI), Pfizer, Inc., 10770 Science Center Dr., San Diego, CA 92121, USA., Stephanie A., Smider, Vaughn V., Felding, Brunhilde H., SinhaCurrent address: Laboratory of Molecular and Cellular Neuroscience, The Rockefeller University, 1230 York Avenue, New York, NY 10065, USA., Subhash C.
Chemical communications 2017 v.53 no.30 pp. 4234-4237
cell growth, chemical compounds, chemical reactions, cytotoxins, drugs, integrins, mutants, neoplasm cells
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.