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| http://dx.doi.org/10.1111/jdv.16953 | DOI Listing |
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Amiloride sensitizes prostate cancer cells to the reversible tyrosine kinase inhibitor lapatinib by modulating Erbb3 subcellular localization.
Cell Mol Life Sci
December 2024
Research Service, VA Northern California Health Care System, Mather, CA, USA.
Neoadjuvant therapy (NAT) has been studied in clinically localized prostate cancer (PCa) to improve the outcomes from radical prostatectomy (RP) by 'debulking' of high-risk PCa; however, using androgen deprivation therapy (ADT) at this point risks castration resistant PCa (CRPC) clonal proliferation. Our goal is to identify alternative NAT that reduce hormone sensitive PCa (HSPC) without affecting androgen receptor (AR) transcriptional activity. PCa is associated with increased expression and activation of the epidermal growth factor receptor (EGFR) family, including HER2 and ErbB3.
View Article and Find Full Text PDFNeuroprotective effects of testosterone on sevoflurane-induced neurotoxicity in testosterone-deprived male mice.
Neuropharmacology
March 2025
Department of Anesthesiology, Tianjin Medical University General Hospital, Tianjin Institute of Anesthesiology, Tianjin, China. Electronic address:
This study aims to investigate whether androgen deprivation, simulating conditions of aging or disease-induced low testosterone levels, increases the susceptibility of male mice to sevoflurane neurotoxicity, and whether testosterone supplementation can reverse the toxic effects of sevoflurane. In here, young male mice were subjected to orchiectomy (ORC) to induce testosterone deprivation. Various techniques, including western blotting, immunofluorescence, Morris Water Maze, Golgi staining, and neuronal signal measurement, were used to evaluate the effects of sevoflurane on long-term (ORC 10 weeks) and short-term (ORC 2 weeks) testosterone deprivation, and assess whether testosterone (1 mg/kg 1 h before sevoflurane exposure) could mitigate sevoflurane-induced neurotoxicity.
View Article and Find Full Text PDFmiR-449, identified through antiandrogen exposure, mitigates functional biomarkers associated with ovarian cancer risk.
Sci Rep
December 2024
Department of Obstetrics and Gynecology, University of Arizona, Tucson, AZ, USA.
The involvement of the androgen receptor (AR) pathway in developing epithelial ovarian cancer is increasingly acknowledged. However, the specific mechanisms by which anti-androgen agents, such as flutamide, may prevent ovarian cancer and their efficacy remain unknown. This study was initiated by investigating the impact of flutamide on miRNA expression in women at high risk (HR) for ovarian cancer.
View Article and Find Full Text PDFDiscovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer.
Eur J Med Chem
January 2025
State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China. Electronic address:
The clinical development of PROTACs targeting the androgen receptor (AR) for degradation has made significant progress. However, effective treatments for metastatic prostate cancers containing the androgen receptor splice variant 7 (AR-V7), a constitutively active mutant without the ligand-binding domain (LBD), are still lacking. Here, we reported the identification of a highly potent, noncovalent PROTAC targeting the N-terminal domain (NTD) of AR, NP18, which is developed from the covalent AR-NTD antagonist EPI-002, and effectively degrades both AR-FL and AR-V7 in 22Rv1 cells (DC: 18 and 26 nM respectively).
View Article and Find Full Text PDFEnhancing screening rates for bone health management in prostate cancer patients on androgen deprivation therapy with an automated outpatient system.
Sci Rep
November 2024
Department of Urology, Taichung Veterans General Hospital, 1650 Taiwan Boulevard Sect. 4, 407219, Taichung, Taiwan, ROC.
Article Synopsis
- * An auto-recruit system was implemented to remind physicians to screen for bone health, resulting in an increase in DXA screening rates from 9.5% to 33.6% within a year.
- * Patients on ADT for longer than a year showed worse bone health, but after screenings, there was a significant rise in the use of supplements for bone health, indicating improved patient management and awareness.
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