Methods and compositions for inhibiting neddylation of proteins
US9447156B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 16, 2012 |
| Grant date | Sep 20, 2016 |
| Priority date | — |
| Expiry date | May 16, 2032 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/04
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
Provided herein is a novel binding pocket within NEDD8 co-E3 proteins that binds NEDD8 E2 enzymes. Particularly at its M-Terminus. Methods are provided for screening for compounds that bind to the disclosed E2-binding pocket in NEDD8 co-E3 proteins. Compounds that bind to the E2-binding pocket and optionally inhibit the activity of NEDD8 co-E3 proteins and pharmaceutical compositions comprising the same are further provided. The NEDD8 co-E3 inhibitors find use, as agents preventing the NEDDylation of a target protein, in inhibiting cell growth and methods for treating cancers, inflammatory disorders, and pathogenic infections. The preferred inhibitors are peptides corresponding to a M-terminal fragment of Dnc1, e.g. MTLASKLKRDD, MLKLRQLQKKKQ, and MIKLFSLKQQKK, which are substituted at the M-Terminus with an uncharged group (e.g. acyl).
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.