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:
Sep. 06, 2022
Filed:
Oct. 10, 2019
Inhibitors of grb2-associated binding protein 1 (gab1) and methods of treating cancer using the same
Arizona Board of Regents on Behalf of the University of Arizona, Tucson, AZ (US);
Board of Regents, the University of Texas System, Austin, TX (US);
Emmanuelle J. Meuillet, Tucson, AZ (US);
Shuxing Zhang, Houston, TX (US);
Lu Chen, Houston, TX (US);
Arizona Board of Regents on Behalf of the University of Arizona, Tucson, AZ (US);
Board of Regents, The University of Texas System, Austin, TX (US);
Abstract
Identification and evaluation of a set of first-in-class potent inhibitors targeting a new cancer target, Grb2-associated binder-1 (GAB1), which integrates signals from different signaling pathways and is frequently over-expressed in cancer cells. Intensive computational modeling is utilized to understand the structure of the GAB1 pleckstrin homology (PH) domain and screened five million compounds. Upon biological evaluation, several inhibitors were found that induced large conformational changes of the target structure exhibited strong selective binding to GAB1 PH domain. Particularly, these inhibitors demonstrated potent and tumor-specific cytotoxicity in breast cancer cells. This targeting GAB1 signaling may be used for cancer therapy, especially for triple negative breast cancer patients.