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SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth.

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 ?v?3/?v?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.

SUBMITTER: Roy S

PROVIDER: S-EPMC6594371 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth.

Roy Saumya S Axup Jun Y JY Forsyth Jane S JS Goswami Rajib K RK Hutchins Benjamin M BM Bajuri Krishna M KM Kazane Stephanie A SA Smider Vaughn V VV Felding Brunhilde H BH Sinha Subhash C SC

Chemical communications (Cambridge, England) 20170401 30

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 ...[more]

PMID: 28357420

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