Department of Experimental Pathology, "Alma Mater Studiorum" University of Bologna, via San Giacomo 14, 40126-Bologna, Italy.
Toxins (Basel). 2011 Jun;3(6):697-720. doi: 10.3390/toxins3060697. Epub 2011 Jun 22.
Ribosome-inactivating proteins (RIPs) are a family of plant toxins that permanently damage ribosomes and possibly other cellular substrates, thus causing cell death. RIPs are mostly divided in two types: Type 1 RIPs that are single-chain enzymatic proteins, and type 2 RIPs that consist of an active A chain (similar to a type 1 RIP) linked to a B chain with lectin properties. RIP-containing conjugates have been used in many experimental strategies against cancer cells, often showing great efficacy in clinical trials. Saporin-S6, a type 1 RIP extracted from Saponaria officinalis L. seeds, has been extensively utilized to construct anti-cancer conjugates because of its high enzymatic activity, stability and resistance to conjugation procedures, resulting in the efficient killing of target cells. This review summarizes saporin-S6-containing conjugates and their application in cancer therapy, considering in-vitro and in-vivo studies both in animal models and in clinical trials. The review is structured on the basis of the targeting of hematological versus solid tumors and on the antigen recognized on the cell surface.
核糖体失活蛋白(RIPs)是一类植物毒素,可永久性地破坏核糖体和其他可能的细胞底物,从而导致细胞死亡。RIPs 主要分为两类:一类是单链酶蛋白的 1 型 RIPs,另一类是由具有凝集素特性的 B 链连接的活性 A 链(类似于 1 型 RIPs)组成的 2 型 RIPs。含有 RIP 的缀合物已被用于许多针对癌细胞的实验策略中,在临床试验中常常显示出很好的疗效。皂素-S6 是一种从皂角种子中提取的 1 型 RIP,由于其高酶活性、稳定性和对缀合过程的抗性,已被广泛用于构建抗癌缀合物,从而有效地杀死靶细胞。本综述总结了含有皂素-S6 的缀合物及其在癌症治疗中的应用,同时考虑了动物模型和临床试验中的体外和体内研究。综述是基于针对血液肿瘤与实体瘤的靶向性以及细胞表面上识别的抗原进行组织的。