The present invention pertains to a complex including nanoparticles and, carried on the surface of the nanoparticles, a lysosomal enzyme inhibitor or kinase inhibitor shown by general formula (A) and a phospholipid mimetic substance shown by general formula (B).
In general formula (A), n1 is an integer of 2-30, n2 is an integer of 2-30, the -S- terminal is a nanoparticle-carrying site, and R10 is a suicide substrate site or a kinase inhibition site. In general formula (B), n3 is an integer in the range of 2-30, and the -S- terminal is a nanoparticle-carrying site. The present invention provides a versatile system capable of efficiently delivering a drug to endolysosomes and allowing the drug to function at a low concentration on lysosomal enzymes, and an anticancer agent in which this system is used.
本发明涉及一种复合物,包括纳米颗粒和纳米颗粒表面携带的通式(A)所示的溶酶体酶
抑制剂或激酶
抑制剂以及通式(B)所示的
磷脂模拟物质。
通式(A)中,n1 为 2-30 的整数,n2 为 2-30 的整数,-S- 端为纳米粒子携带位点,R10 为自杀底物位点或激酶抑制位点。通式(B)中,n3 是 2-30 范围内的整数,-S- 端是纳米粒子携带位点。本发明提供了一种多功能系统,能够有效地将药物输送到内溶酶体,并使药物以低浓度作用于溶酶体酶,还提供了一种使用该系统的抗癌剂。