SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth

被引：9

作者：

Roy, Saumya ^{[1
]}

Axup, Jun Y. ^{[1
]}

Forsyth, Jane S. ^{[2
]}

Goswami, Rajib K. ^{[1
,3
]}

Hutchins, Benjamin M. ^{[1
]}

Bajuri, Krishna M. ^{[1
]}

Kazane, Stephanie A. ^{[1
,4
]}

Smider, Vaughn V. ^{[1
]}

Felding, Brunhilde H. ^{[2
]}

Sinha, Subhash C. ^{[1
,5
]}

机构：

[1] Scripps Res Inst, Dept Cell & Mol Biol, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Dept Chem Physiol, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA

[3] Indian Assoc Cultivat Sci, Dept Organ Chem, Kolkata, India

[4] Pfizer Inc, Ctr Therapeut Innovat, 10770 Sci Ctr Dr, San Diego, CA 92121 USA

[5] Rockefeller Univ, Lab Mol & Cellular Neurosci, 1230 York Ave, New York, NY 10065 USA

来源：

CHEMICAL COMMUNICATIONS | 2017年 / 53卷 / 30期

关键词：

INTEGRIN; IMMUNOTOXINS; EXPRESSION;

D O I：

10.1039/c7cc00745k

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：4234 / 4237

页数：4

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