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New Promising Steroidal Aromatase Inhibitors with Multi-Target Action on Estrogen and Androgen Receptors for Breast Cancer Treatment.
Cancers (Basel)
January 2025
UCIBIO-Applied Molecular Biosciences Unit, Laboratory of Biochemistry, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto, Portugal.
Endocrine therapies that comprise anti-estrogens and aromatase inhibitors (AIs) are the standard treatment for estrogen receptor-positive (ER+) (Luminal A) breast cancer-the most prevalent subtype. However, the emergence of resistance restricts their success by causing tumor relapse and re-growth, which demands a switch towards other therapeutic approaches in order to minimize or overcome resistance. Indeed, this clinical limitation highlights the search for new molecules to improve cancer treatment.
View Article and Find Full Text PDFDiscovery of -(1,2,4-Thiadiazol-5-yl)benzo[]oxepine-4-carboxamide Derivatives as Novel Antiresistance Androgen Receptor Antagonists.
J Med Chem
January 2025
State Key Laboratory of Advanced Drug Delivery and Release Systems, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
The ligand-binding pocket of the androgen receptor (AR) is the targeting site of all clinically used AR antagonists. However, various drug-resistant mutations emerged in the pocket. We previously reported a new targeting site at the dimer interface of AR (dimer interface pocket) and identified a novel antagonist M17-B15 that failed in oral administration.
View Article and Find Full Text PDFUnveiling the Potential of S4 on Non-small Cell Lung Cancer Cells: Impact on Proliferation, Apoptosis, Senescence, and Metabolome Profile.
Anticancer Agents Med Chem
January 2025
School of Medicine, Muğla Sıtkı Koçman University, Muğla, Turkey.
Background: Lung cancer is a highly aggressive tumor with limited therapeutic options. The misregulation of Androgen Receptor (AR) signaling has been observed in lung cancer. Therefore, inhibiting AR signaling is a promising strategy for treating lung cancer.
View Article and Find Full Text PDFIntegrative Bioinformatics and Experimental Validation Reveal the Mechanistic Action of Patchouli Alcohol in Prostate Cancer Treatment.
Curr Pharm Biotechnol
January 2025
Department of Urology & Andrology, Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu 610072, Sichuan.
Introduction: Prostate cancer is an androgen-dependent malignancy, and the use of androgen deprivation therapies frequently results in treatment resistance, relapse, and the development of aggressive castration-resistant tumors. Patchouli alcohol, a tricyclic sesquiterpene derived from Pogostemon cablin of the Labiatae family, has demonstrated potential in modulating inflammatory responses and tumor progression. This study aimed to investigate the mechanisms through which patchouli alcohol influences inflammatory pathways associated with prostate cancer using bioinformatics and experimental validation.
View Article and Find Full Text PDFEffect of hydro-ethanol extract of Caesalpinia pulcherrima (L.) Sw. leaves in human and rat: In vitro approach of male contraceptive development.
JBRA Assist Reprod
January 2025
Molecular Medicine, Nutrigenomics and Public Health Research Laboratory, Department of Bio-Medical Laboratory Science and Management, Vidyasagar University, Midnapore 721 102, West Bengal, India.
Objective: The study focused the contraceptive efficacy of hydro-ethanolic (60:40) extract (HEE) of Caesalpinia pulcherrima leaves in human and rat sperm samples by in vitro study.
Methods: Six young fertile adult males were selected for semen collection. Sperm samples were collected from six adult rat also by chopping the epididymis along with the collection of testicles, epididymis, and liver.
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