Anticancer agents based on regulation of protein prenylation
US7423170B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 23, 2006 |
| Grant date | Sep 9, 2008 |
| Priority date | — |
| Expiry date | May 27, 2026 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/091
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.