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Full-Text Articles in Medical Molecular Biology
Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi
Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi
Student Scholar Symposium Abstracts and Posters
The development of prostate cancer (PCa) relies strongly on the activation of the androgen receptor (AR) signaling pathway by its natural ligand dihydrotestosterone. Furthermore, PCa progression to metastatic disease represents oncogene addiction to AR activity. Androgen ablation therapy is thus a mainstay therapy against this disease, but the development of ligand-independent AR activation and persisting AR expression eventually leads to castration resistant PCa (CRPC). Therefore, down-regulation of AR expression in PCa cells may be an effective therapeutic modality. The diarylpentanoid ca27 has previously been shown to down-regulate AR expression by an unknown mechanism of action. The present work represents a …
Mechanisms Of Therapeutic Resistance In Castration Resistant Prostate Cancer, Sarah Katherine Martin
Mechanisms Of Therapeutic Resistance In Castration Resistant Prostate Cancer, Sarah Katherine Martin
Theses and Dissertations--Molecular and Cellular Biochemistry
Taxane based chemotherapy is an effective treatment for castration-resistant prostate cancer (CRPC) via stabilization of microtubules. Progression to castration-resistant prostate cancer is characterized by increased androgen receptor (AR), elevated intra-prostatic androgens and activated AR signaling despite castrate levels of androgens.
Previous studies identified that the inhibitory effect of microtubule targeting chemotherapy on AR activity was conferred by interfering with AR intracellular trafficking. The N-terminal domain (NTD) of AR was identified as a tubulin interacting domain that can be effectively targeted by the novel small molecular inhibitor, EPI. Taken together, this evidence provided the rationale that targeting AR nuclear translocation and …