申请人:H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
公开号:US10329326B2
公开(公告)日:2019-06-25
The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
本发明涉及一种修饰的 MC1R 多肽配体,该配体包括一种黑色素皮质素 1 受体(MC1R)配体多肽和一种用于与表面或制剂共轭的官能团或连接体,例如点击官能团。经修饰的 MC1R 肽配体可通过附带互补点击官能团的点击反应等方式与分子偶联,形成 MC1R 靶向制剂。药物、造影剂、聚合物、颗粒、胶束、较大结构的表面或其他分子都可以靶向 MC1R。本发明还涉及一种 MC1R 肽配体-胶束复合物,该复合物包括通过点击反应产物与胶束连接的黑色素皮质素 1 受体配体肽。该胶束在体内稳定,可通过多肽配体与 MC1R 或肿瘤的结合靶向黑色素瘤肿瘤细胞,并选择性地向肿瘤细胞提供可检测和/或治疗剂(如可成像的造影剂和/或抗癌剂)。