Document Type
Patent
Publication Date
June 2015
Patent Number
9045434
CPC
C07D 233/64(20130101), A61K 31/4174(20130101)
Abstract
A compound and method for treating myocilin glaucoma using a selective Grp94 inhibitor is presented. Clearance of mutant myocilin can be promoted by selectively targeting the endoplasmic reticulum (ER) chaperone Grp94 using siRNA knockdown or small molecule inhibitors. Grp94 contributes to the intracellular accumulation of mutant myocilin. Tailored treatments aimed at disrupting the Grp94/mutant myocilin interaction can be used as a new therapeutic strategy for myocilin glaucoma. The inventors developed a compound having a general backbone structure of geldanamycin (GDA) and radicicol (RDC) in which a more hydrophobic surrogate of the quinone in GDA is linked to the resorcinol in RDC through a cis-amide bioisostere.
Application Number
14/083,031
Recommended Citation
Dickey, Chad Anthony; Suntharalingam, Amirthaa; and Blagg, Brian S. J., "Compositions and methods of treatment for myocilin glaucoma by selectively inhibiting GRP94" (2015). USF Patents. 29.
https://digitalcommons.usf.edu/usf_patents/29
Assignees
University of South Florida
Filing Date
11/18/2013
