Enhancements    

Next Generation FKBP52 Targeting Drugs for the Treatment of Prostate and Breast Cancer

Next Generation FKBP52 Targeting Drugs for the Treatment of Prostate and Breast Cancer
Inventors: Marc Cox, Artem Cherkasov, Fuqiang Ban
Patent No. 11,878,961

Description:
Prostate cancer is the most common cancer among men in several countries, which have presented 1.3 million new cases in 2018 alone1. The chaperon proteins of the cancer patients facilitate both the dynamic protein folding, unfolding, organization, and degradation through ATP-dependent cycles of binding and releasing for the protein’s function. One family of such chaperones are FK506-binding proteins (FKBPs); FKBPs and cyclophilins (CyP) belong to the immunophilin family that are cellular receptors for immunosuppressant drugs such as FK506, rapamicyn and cyclosporine A (CsA). FKBPs exhibit peptidyl prolyl isomerase (PPIase) activity and catalyze the cis/trans isomerization in protein folding process in the cytoplasm, and have important roles of protein stability, protein trafficking, receptor signaling and others.

Abstract:
We previously identified our first FKBP52 targeting drug, GMC1, through an in silico screen and patented that molecule for use in treating breast and prostate cancer. We have now performed a much broader in silico screen and have identified completely new chemotypes that can and should be pursued independently of GMC1. See the attached document for more details.

Issue Date: 01/23/2024
Application Date: 01/20/2021
Post Date: 02/13/2020

UTEP Docket No: 2020-008