The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 13, 2018

Filed:

Oct. 21, 2014
Applicants:

European Molecular Biology Laboratory (Embl), Heidelberg, DE;

Universite Grenoble Alpes, Saint Martin d'Heres, FR;

Centre National DE LA Recherche Scientifique, Paris, FR;

Inventors:

Denis Bouvier, Meylan, FR;

Thibaut Crepin, Grenoble, FR;

Rob Ruigrok, Sassenage, FR;

Aelxander Dias, Voiron, FR;

Stephen Cusack, Seyssinet-Pariset, FR;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C12N 9/22 (2006.01); A61K 31/192 (2006.01); C12N 9/12 (2006.01); C12Q 1/44 (2006.01); G06F 19/12 (2011.01); G06F 19/16 (2011.01);
U.S. Cl.
CPC ...
C12N 9/22 (2013.01); A61K 31/192 (2013.01); C12N 9/127 (2013.01); C12Q 1/44 (2013.01); G06F 19/12 (2013.01); G06F 19/16 (2013.01); C07K 2299/00 (2013.01); G01N 2333/922 (2013.01); G01N 2500/02 (2013.01);
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.


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