The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
本发明的前药是治疗剂的改良形式,包括治疗剂、寡肽、稳定基团和可选的连接基团。该前药可被Thimet寡肽酶或TOP酶
水解。本发明还揭示了通过利用共轭物中可被TOP酶
水解的序列设计前药的方法以及使用本发明的前药治疗患者的方法。