Voltage Gated Sodium Channel Blockers as Treatment for Prostate Cancer
- 技术优势
- Sodium channel blockers represent a novel approach to the treatment of prostate cancer.Fluorescent moieties allow for these compounds to be traced in assays for the diagnosis of prostate cancer. Fluorescent moieties enable the visualization of compounds reaching the treatment target. Isoform specific Nav can be used as biomarkers to identify the stage of prostate cancer.
- 详细技术说明
- Voltage Gated Sodium Channels (VGSC or Nav) with known expression incentral nervous and cardiac tissue are present in human prostatecancer. This invention encompasses novel sodium channel blockers thatinhibit both androgen dependent and independent human prostate cancer.These blockers down-regulate the expression of certain Nav isoform(s)relevant to prostate cancer. Structure Analysis Relationship (SAR) hasdemonstrated a significant correlation with Nav isoform selectivity. Intumors from prostate cancer patients, a correlation between GleasonScore and isoform specificity has been elucidated, which has led toidentification of specific Nav isoforms as biomarkers for prostatecancer. The results of this research demonstrate the potential of Navtargeted therapies for the treatment and diagnosis of human prostatecancer.
- *Abstract
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- *Publications
- No references or resources available.
- *Stage of Development
- A lead compound was evaluated against a human tumor xenograft model and a 70% reduction in tumor volume was observed.Compoundstability studies, including metabolic studies using human livermicrosomes by LCMS detection, are currently in progress.
- 国家/地区
- 美国
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