SMI-核糖体失活蛋白缀合物选择性抑制肿瘤细胞生长。
SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth.
作者信息
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
机构信息
Department of Cell and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
出版信息
Chem Commun (Camb). 2017 Apr 11;53(30):4234-4237. doi: 10.1039/c7cc00745k.
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 αβ/αβ, 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.
摘要
使用核糖体失活蛋白（RIP）皂草素6的细胞靶向缀合物，是通过皂草素丙氨酸157半胱氨酸突变体、整合素αβ/αβ的小分子抑制剂（SMI）以及强效细胞毒素奥瑞他汀F（AF）制备而成。这些缀合物选择性且强效地抑制表达靶整合素的肿瘤细胞的增殖。我们预计小分子-RIP生物缀合物方法可广泛应用于其他小分子药物。
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