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Pharmaceutical Compositions Which Inhibit Fkbp52-Mediated Regulation of Androgen Receptor Function and Methods of Using Same
Inventors: Marc Cox, Leonard M. Neckers, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Kugelman-Tonos, Heather A. Balsiger, Robert Fletterick
Description:This patent application embodies pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52. MJC13 is a first-in-class drug for targeting the regulation of androgen receptor (AR) by FKBP52. Through binding a recently identified regulatory surface on AR (BF3), MJC13 prevents the FKBP52-receptor complex from dissociating resulting in the retention of AR in the cytoplasm. MJC13 was shown to effectively block AR signaling and AR-dependent cancer cell proliferation in a variety of human prostate cancer cell lines, and preclinical studies demonstrate impressive effects on tumor growth in a prostate cancer xenograft model. Abstract:Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.
Issue Date: 10/10/2017 Application Date: 12/15/2015 Post Date: 04/27/2018
UTEP Docket No: 2009-014
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