Melanocortin 1 receptor ligands and methods of use

US10329326B2 · kind B2 · utility

Assignees

• Arizona Board of Regents on Behalf of the University of Arizona · US
• The Board of Regents of the University of Texas System · US
• H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE INC. · US
• Intezyne Technologies Inc. · US

Inventors

• Robert J. Gillies · Tampa, US
• David L. Morse · Tampa, US
• Natalie M. Barkey · Tampa, US
• Kevin N. Sill · Tampa, US
• Josef Vagner · Tucson, US
• Narges K. Tafreshi · Tampa, US
• Jonathan L. Sessler · Austin, US
• Christian Preihs · Austin, US
• Victor J. Hruby · Tucson, US

Key dates

• Filing date: Sep 12, 2016
• Grant date: Jun 25, 2019
• Expiry date: Sep 12, 2036

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/34
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.