Influenza A 2009 pandemic H1N1 polypeptide fragments comprising endonuclease activity and their use
US9181307B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 15, 2011 |
| Grant date | Nov 10, 2015 |
| Priority date | — |
| Expiry date | Mar 15, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12N2760/16122
- 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 possessing endonuclease activity, wherein said PA subunit is from Influenza A 2009 pandemic H1N1 virus or is a variant thereof. 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 which are able to modulate, preferably to inhibit, the endonuclease activity of the PA subunit polypeptide fragment or variant thereof of the present invention and pharmaceutical compositions comprising said compounds for the treatment of di…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.