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. 01, 2019
Filed:
Dec. 12, 2014
The Board of Regents of the University of Texas System, Austin, TX (US);
David T. Chuang, Dallas, TX (US);
Shih-Chia Tso, Carrolton, TX (US);
Xiangbing Qi, Beijing, CN;
Wen-Jun Gui, Dallas, TX (US);
Cheng-Yang Wu, Dallas, TX (US);
Jacinta L. Chuang, Dallas, TX (US);
Uttam K. Tambar, Dallas, TX (US);
R. Max Wynn, Hurst, TX (US);
The Board of Regents of the University of Texas System, Austin, TX (US);
Abstract
The present disclosure relates to the identification of PDK inhibitors and their use in the treatment of diseases such as diabetes, cardiovascular disease and cancer. The invention relates to the development of robust PDK inhibitors that can be used to improve glucose metabolism and correct metabolic dysfunction in vivo. Based on the unique structural features present in the ATP-binding pocket of PDK2, a single functional-group change was made in a known Hsp90 inhibitor that binds to the corresponding pocket of the latter protein from the GHKL family. This approach efficiently converted the Hsp90 inhibitor to a highly specific inhibitor for all PDK isoforms. These final PDK inhibitors of this series robustly augments PDC activity with reduced phosphorylation in tissues.