申请人:National University Corporation Hokkaido University
公开号:US20200138973A1
公开(公告)日:2020-05-07
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.
本发明涉及一种包括纳米粒子的复合物,所述纳米粒子表面携带有一种由通用式(A)显示的溶酶体酶抑制剂或激酶抑制剂以及一种由通用式(B)显示的磷脂类拟物物质。
在通用式(A)中,n1是2-30的整数,n2是2-30的整数,-S-端是纳米粒子携带位点,R10是自杀底物位点或激酶抑制位点。在通用式(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,能够有效地将药物传递至内溶酶体,并使药物在低浓度下对溶酶体酶起作用,以及使用该系统的抗癌剂。