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.
Patent No.:
Date of Patent:
Jan. 06, 2015
Filed:
Aug. 04, 2010
Dionisios Rentzeperis, Downingtown, PA (US);
Marta Cristina Abad, Downingtown, PA (US);
Ludmila A. Barnakova, Downingtown, PA (US);
Frank A. Lewandowski, Washington Crossing, PA (US);
Cynthia M. Milligan, Rutledge, PA (US);
Dionisios Rentzeperis, Downingtown, PA (US);
Marta Cristina Abad, Downingtown, PA (US);
Ludmila A. Barnakova, Downingtown, PA (US);
Frank A. Lewandowski, Washington Crossing, PA (US);
Cynthia M. Milligan, Rutledge, PA (US);
Janssen Pharmaceutica N.V., Beerse, BE;
Abstract
The crystal structure of the ligand binding domain of ERR-α in complex with a ligand that forms a reversible thioether bond to Cys325 of ERR-α, methods to measure dissociation rates for ligands that form reversible covalent bonds, and methods to design ligands that form reversible covalent bonds for use as modulators of ERR-α activity are disclosed. The crystal structure and methods provide a novel molecular mechanism for modulation of the activity of ERR-α and provide the basis for rational drug design to obtain potent specific ligands for use as modulators of the activity of this new drug target.