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:
Jul. 03, 2012
Filed:
Jan. 12, 2010
Michael R. Downes, San Diego, CA (US);
Mark A. Verdicia, New York, NY (US);
Joseph P. Noel, San Diego, CA (US);
Ronald M. Evans, La Jolla, CA (US);
Lindsey J. Bowman, San Diego, CA (US);
Marianne Bowman, San Diego, CA (US);
Michael R. Downes, San Diego, CA (US);
Mark A. Verdicia, New York, NY (US);
Joseph P. Noel, San Diego, CA (US);
Ronald M. Evans, La Jolla, CA (US);
Lindsey J. Bowman, San Diego, CA (US);
Marianne Bowman, San Diego, CA (US);
The Salk Institute for Biological Studies, La Jolla, CA (US);
Abstract
The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a time-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR. The present invention further provides compositions comprising compounds identified by such invention methods.