A Novel Treatment for Metastatic Prostate Cancer

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Castration-resistant prostate cancer (CRPC) is currently incurable and makes prostate cancer the second most common cause of cancer death among men in the United States.
Innovators at the University of Pittsburgh have identified novel small molecules that bind to the androgen receptor (AR) and block the nuclear localization and function of AR in CRPC cells.
Multiple studies have shown that the androgen receptor (AR) is activated via multiple mechanisms including AR overexpression, mutation, hypersensitization, and/or intratumoral androgen synthesis in patients relapsed after androgen deprivation therapy (ADT).
A structure-guided computational approach was used to identify allosteric druggable sites in PTHR and to predict compounds that would bind to this site, and Pitt researchers discovered four small-molecule compounds that act as negative allosteric modulators of PTHR signaling.
Parathyroid hormone (PTH) type 1 receptor (PTHR) is an indispensable G protein-coupled receptor (GPCR) of class B that functions to regulate blood levels of vitamin D, calcium, and phosphate ions in the body, as well as bone turnover.
A structure-guided computational approach was used to identify allosteric druggable sites in PTHR and to predict compounds that would bind to this site, and Pitt researchers discovered four small-molecule compounds that act as negative allosteric modulators of PTHR signaling.
B signaling pathway and responses of the same cell types to a library of bioactive compounds.
From the 717 initial hit compounds, docking studies were carried out in silico on key targets in the TNF receptor identifying three compounds of interest.
From the 717 initial hit compounds, docking studies were carried out in silico on key targets in the TNF receptor identifying three compounds of interest.
    • Technology Type
      • 21
        Therapeutic Modality
      • 2
        Diagnostic/Assay
      • 1
        Digital Health
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    • Technology Subtype
      • 17
        Small Molecule
      • 2
        Gene Therapy - RNA
      • 1
        Antibody - mAb
      • 1
        Biomarker
      • 1
        Digital Therapeutic
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    • Therapeutic Areas
      • 14
        Oncology
      • 4
        Infectious Disease
      • 2
        Nephrology
      • 2
        Neuroscience
      • 1
        Cardiovascular
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    • Therapeutic Indications
      • 2
        Liver cancer
      • 2
        Prostate cancer
      • 1
        Acute Kidney Injury (AKI)
      • 1
        Alzheimer's Disease
      • 1
        Breast cancer
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    • Tags
      • 4
        Small molecule
      • 2
        Aging
      • 2
        Immuno-oncology
      • 2
        Life Science
      • 1
        Antibody - mAb
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    • Lead Inventor
      • 2
        Kazunori Koide
      • 2
        Thomas Smithgall
      • 2
        Xiaosong Wang
      • 1
        Alexander Deiters
      • 1
        Alexander Doemling
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    • Department
      • 4
        Chemistry
      • 3
        Med-Pathology
      • 2
        Med-Computational and Systems Biology
      • 2
        Med-Medicine
      • 2
        Med-Microbiology and Molecular Genetics
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    • All Tech Innovators
      • 2
        Alexander Deiters
      • 2
        Allen B. Reitz
      • 2
        Ivet Bahar
      • 2
        Kari Nichole Nejak-Bowen
      • 2
        Kazunori Koide
      • Add ...
    • Date Submitted
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