Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
US10047122B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 14, 2014 |
| Grant date | Aug 14, 2018 |
| Priority date | — |
| Expiry date | Mar 14, 2034 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K2319/50
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.