申请人:CHU SHAOSONG
公开号:WO2015187540A1
公开(公告)日:2015-12-10
Peptide-drug conjugates comprising p-aminobenzyl carbamoyl or p-aminobenzolyl carbonate self-immolating linkers are disclosed. The peptide-drug conjugates comprise a peptide moiety that can be cleaved by cellular proteases, bound to the self-immolating linker, which linker is bound to a cytotoxic drug moiety. Upon cleavage of the peptide moiety, the linker self- immolates, releasing the cytotoxic drug in active form. Dimeric structures of the peptide drug conjugates comprising two molecules of cytotoxic drug per conjugate are also disclosed.
肽-药物共轭物包括p-氨基苯甲酰基或p-氨基苯酰基碳酸酯自解链。这些肽-药物共轭物包括一个可以被细胞蛋白酶裂解的肽基团,与自解链结合,该链结合到一个细胞毒性药物基团。在肽基团被裂解后,链自解,释放活性形式的细胞毒性药物。还公开了包含每个共轭物中两分子细胞毒性药物的肽药物共轭物的二聚体结构。