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
Department of Cell and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Chem Commun (Camb). 2017 Apr 11;53(30):4234-4237. 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 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.
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。
