Polypeptide fragments comprising endonuclease activity and their use
US9890368B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Oct 21, 2014 |
| Grant date | Feb 13, 2018 |
| Priority date | — |
| Expiry date | Oct 21, 2034 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/02
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention relates to polypeptide fragments comprising an amino-terminal fragment of the PA subunit of a viral RNA-dependent RNA polymerase or variants thereof possessing endonuclease activity, wherein said PA subunit is from a virus belonging to the Orthomyxoviridae family. This invention also relates to (i) crystals of the polypeptide fragments which are suitable for structure determination of said polypeptide fragments using X-ray crystallography and (ii) computational methods using the structural coordinates of said polypeptide to screen for and design compounds that modulate, preferably inhibit the endonucleolytically active site within the polypeptide fragment. In addition, this invention relates to methods identifying compounds that bind to the PA polypeptide fragments possessing endonuclease activity and preferably inhibit said endonucleolytic activity, preferably in a high throughput setting. This invention also relates to compounds and pharmaceutical compositions comprising the identified compounds for the treatment of disease conditions due to viral infections caused by viruses of the Orthomyxoviridae family.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.