Description:
Project ID: TECH-2025-20
Background
Every 16 mins a man will die of Prostate cancer. Bone metastasis is the predominant cause of morbidity and mortality in prostate cancer, with > 80 % of lethal cases exhibiting skeletal involvement. Parathyroid hormone-related protein (PTHrP), secreted by tumor cells, binds and activates PTH1R on osteoblasts and cancer cells, driving osteolysis and tumor growth (“vicious cycle”). There exists no small-molecule on the market which can eliminate PTH1R directly. PROTACs, heterobifunctional molecules linking a target-binding moiety to an E3-ligase recruiter, offer catalytic, selective protein degradation and can target proteins previously deemed “undruggable,” including class B GPCRs such as PTH1R.
Invention Description
Researchers at the University of Toledo have developed novel PTH1R PROTACs for treatment of bone metastases in drug resistant prostate cancer.
Applications
Treatment of advanced metastasizing prostate cancer
Advantages
- Specific degradation of PTHrP-activated PTH1R without impact on PTH-activated PTH1R
- Blocking PTH1R inhibits prostate cancer metastases
- Avoids resistance issues of AR inhibitors
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IP Status: Patent Pending
