Genetically-encoded macrocyclic peptide libraries bearing a pharmacophore
US12416101B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Nov 28, 2019 |
| Grant date | Sep 16, 2025 |
| Priority date | — |
| Expiry date | Jan 30, 2042 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC40B30/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention relates to a method of forming a macrocyclic peptide bearing a pharmacophore and said produced macrocyclic peptide, wherein the method comprises the steps of: reacting a peptide with two thiol groups of cysteine side chains with the reactive compound 1,5-dichloropentanedion-2,4. The reaction between the reactive compound and the peptide produces an 1,3-diketone-containing macrocyclic polypeptide. The macrocycle with a 1,3-diketone group is then modified by reaction of said macrocycle with an alkyl or aryl hydrazine group bearing a pharmacophore in benign aqueous conditions. The macrocycles may be displayed in a library, such as a phage display library, and used to biopan for affinity against a selected target.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.