SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growthElectronic supplementary information (ESI) available: Synthesis of compounds 3 and 4, and production and evaluation of the SMI-Sap, SMI(AF)-Sap, and cpAb 38C2-1. See DOI: 10.1039/c7cc00745k

• Main Authors: Roy, Saumya, Axup, Jun Y, Forsyth, Jane S, Goswami, Rajib K, Hutchins, Benjamin M, Bajuri, Krishna M, Kazane, Stephanie A, Smider, Vaughn V, Felding, Brunhilde H, Sinha, Subhash C
• Format: Article
• Language: English
• ISSN: 1359-7345; 1364-548X
• DOI: 10.1039/c7cc00745k

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 α v β 3 /α v β 5 , 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. Cell-targeting conjugates of Saporin 6, prepared using a small molecule inhibitor of integrins α v β 3 and α v β 5 and the Saporin A157C mutant, selectively and potently inhibited proliferation of tumor cells expressing the target integrins.