Stable analogs of bioactive peptides containing disulfide linkages
US6664367B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 21, 1994 |
| Grant date | Dec 16, 2003 |
| Priority date | — |
| Expiry date | Jul 21, 2014 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S930/28
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (—S—S—) is replaced with a monosulfide bond (—S—) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified site is a bifunctional effector molecule. In thioketal expansion, an alkylidene unit (—CR1C2—) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.