Publication number: 20250262317
Abstract: Herein is reported a polypeptide-linker-nucleic acid conjugate, wherein the linker comprises a 3-amino propanamide unit, a 2,6-diamino hexanoic acid amide unit, and a 1,4,5,5a,6,6a,7,8-octahydrocyclopropa[5,6]cycloocta[1,2-d]-1,2,3-triazole unit, wherein the polypeptide comprises a C-terminal lysine residue, and wherein the nucleic acid comprises an oxygen linked to a phosphorous atom of the oxidation state V at 5? or 3? terminus, wherein the 3-amino group of the 3-amino propanamide unit and the carboxy function of the lysine residue of the polypeptide are linked by/form an amide bond, the carboxy function of the 3-amino propanamide unit and the alpha amino group of the 2,6-diamino hexanoic acid amide unit are linked by/form an amide bond, the 6-amino group of the 2,6-diamino hexanoic acid amide unit is a nitrogen of the 1,2,3-triazole element of the 1,4,5,5a,6,6a,7,8-octahydrocyclopropa[5,6]cycloocta[1,2-d]-1,2,3-triazole unit, and the oxygen linked to the phosphorous atom of the nucleic acid is covalently l
Type:
Application
Filed:
January 21, 2025
Publication date:
August 21, 2025
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Kerstin HOFER, Mads MANSØ, Rainer E. MARTIN, Mohamed Yosry Hassan MOHAMED, Tobias OELSCHLAEGEL, Jacob RAVN, Felix Franz SCHUMACHER, Tatjana SELA