SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

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 alpha(v)beta(3)/alpha(v)beta(5), and a potent cytotoxin, auristatin F (AF). The conjugates selectively and potently inhibit...

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Published inChemical communications (Cambridge, England) Vol. 53; no. 30; pp. 4234 - 4237
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 Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 2017
Subjects
Chemistry
Chemistry, Multidisciplinary
Conjugates
Drugs
Inhibition
Inhibitors
Physical Sciences
Proteins
Science & Technology
Tumors
IMMUNOTOXINS
EXPRESSION
INTEGRIN
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Summary: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 alpha(v)beta(3)/alpha(v)beta(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.
Bibliography:NIH RePORTER
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ISSN:1359-7345
1364-548X
DOI:10.1039/c7cc00745k