Uckun F M, Evans W E, Forsyth C J, Waddick K G, Ahlgren L T, Chelstrom L M, Burkhardt A, Bolen J, Myers D E
Department of Therapeutic Radiology-Radiation Oncology, University of Minnesota, Minneapolis 55455.
Science. 1995 Feb 10;267(5199):886-91. doi: 10.1126/science.7531365.
B-cell precursor (BCP) leukemia is the most common form of childhood cancer and the second most common form of acute leukemia in adults. Human BCP leukemia was treated in a severe combined immunodeficient mouse model by targeting of the tyrosine kinase inhibitor Genistein (Gen) to the B cell-specific receptor CD19 with the monoclonal antibody B43. The B43-Gen immunoconjugate bound with high affinity to BCP leukemia cells, selectively inhibited CD19-associated tyrosine kinases, and triggered rapid apoptotic cell death. At less than one-tenth the maximum tolerated dose more than 99.999 percent of human BCP leukemia cells were killed, which led to 100 percent long-term event-free survival from an otherwise invariably fatal leukemia. The B43-Gen immuno-conjugate might be useful in eliminating leukemia cells in patients who have failed conventional therapy.
B细胞前体(BCP)白血病是儿童癌症最常见的形式,也是成人急性白血病第二常见的形式。在严重联合免疫缺陷小鼠模型中,通过用单克隆抗体B43将酪氨酸激酶抑制剂染料木黄酮(Gen)靶向B细胞特异性受体CD19来治疗人类BCP白血病。B43-Gen免疫缀合物与BCP白血病细胞高亲和力结合,选择性抑制与CD19相关的酪氨酸激酶,并引发快速凋亡性细胞死亡。在低于最大耐受剂量十分之一的情况下,超过99.999%的人类BCP白血病细胞被杀死,这使得原本必然致命的白血病实现了100%的长期无事件生存。B43-Gen免疫缀合物可能有助于消除常规治疗失败患者体内的白血病细胞。