Results 21 to 30 of about 17,593 (256)

High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor

Cells, 2020
Prostate cancer is the most commonly diagnosed malignancy in men. Its growth mainly relies on the activity of the androgen receptor (AR), justifying the use of androgen deprivation therapy as a gold standard treatment for the metastatic disease ...
Hadjer Dellal, Abdelhay Boulahtouf, Elina Alaterre, Alice Cuenant, Marina Grimaldi, William Bourguet, Céline Gongora, Patrick Balaguer, Philippe Pourquier   +8 more
doaj   +1 more source

Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists

Frontiers in Chemistry, 2022
Prostate cancer is one of the malignant tumors and the second most common malignant tumor in men. Clinically used androgen receptor (AR)–targeted drugs can antagonize androgen and inhibit tumor growth, but these drugs can cause serious resistance ...
Yueheng Qi, Yueheng Qi, Hong Chen, Shijin Chen, Jianliang Shen, Jingguo Li   +5 more
doaj   +1 more source

Anti-Androgen Receptor Therapies in Prostate Cancer: A Brief Update and Perspective

Frontiers in Oncology, 2022
Prostate cancer is a major health issue in western countries and is the second leading cause of cancer death in American men. Prostate cancer depends on the androgen receptor (AR), a transcriptional factor critical for prostate cancer growth and ...
Jian Huang, Biyun Lin, Benyi Li
doaj   +1 more source

Endocrine disrupting potential of selected azole and organophosphorus pesticide products through suppressing the dimerization of human androgen receptor in genomic pathway

Ecotoxicology and Environmental Safety, 2022
Several pesticides widely used in agriculture have been considered to be endocrine disrupting chemicals through their binding affinities to estrogen or androgen receptors.
Da-Woon Jung, Da-Hyun Jeong, Hee-Seok Lee   +2 more
doaj   +1 more source

Conformational dynamics of androgen receptors bound to agonists and antagonists [PDF]

Scientific Reports, 2021
AbstractThe androgen receptor (AR) is critical in the progression of prostate cancer (PCa). Small molecule antagonists that bind to the ligand binding domain (LBD) of the AR have been successful in treating PCa. However, the structural basis by which the AR antagonists manifest their therapeutic efficacy remains unclear, due to the lack of detailed ...
Gim, Hyo Jin, Park, Jiyong, Jung, Michael E, Houk, KN   +3 more
openaire   +5 more sources

Effect of small molecules modulating androgen receptor (SARMs) in human prostate cancer models.

PLoS ONE, 2013
The management of hormone-refractory prostate cancer represents a major challenge in the therapy of this tumor, and identification of novel androgen receptor antagonists is needed to render treatment more effective.
Anna Tesei, Carlo Leonetti, Marzia Di Donato, Elisa Gabucci, Manuela Porru, Greta Varchi, Andrea Guerrini, Dino Amadori, Chiara Arienti, Sara Pignatta, Giulia Paganelli, Michele Caraglia, Gabriella Castoria, Wainer Zoli   +13 more
doaj   +1 more source

Androgen deprivation restores ARHGEF2 to promote neuroendocrine differentiation of prostate cancer

Cell Death and Disease, 2022
Androgen receptor (AR) plays an important role in the progression of prostate cancer and has been targeted by castration or AR-antagonists. The emergence of castration-resistant prostate cancer (CRPC) after androgen deprivation therapy (ADT) is ...
Xuanrong Chen, Yi Shao, Wanqing Wei, Shimiao Zhu, Yang Li, Yutong Chen, Hanling Li, Hao Tian, Guijiang Sun, Yuanjie Niu, Zhiqun Shang   +10 more
doaj   +1 more source

Interleukin-10 Induces Expression of Neuroendocrine Markers and PDL1 in Prostate Cancer Cells

Prostate Cancer, 2020
Interleukin-10 (IL10) is best studied for its inhibitory action on immune cells and ability to suppress an antitumour immune response. But IL10 also exerts direct effects on nonimmune cells such as prostate cancer epithelial cells.
Abrar Samiea, Jeff S. J. Yoon, Christopher J. Ong, Amina Zoubeidi, Thomas C. Chamberlain, Alice L.-F. Mui   +5 more
doaj   +1 more source

SIRNA-directed in vivo silencing of androgen receptor inhibits the growth of castration-resistant prostate carcinomas. [PDF]

PLoS ONE, 2007
BACKGROUND: Prostate carcinomas are initially dependent on androgens, and castration or androgen antagonists inhibit their growth. After some time though, tumors become resistant and recur with a poor prognosis.
Daniel Compagno, Carole Merle, Aurélie Morin, Cristèle Gilbert, Jacques R R Mathieu, Aline Bozec, Claire Mauduit, Mohammed Benahmed, Florence Cabon   +8 more
doaj   +1 more source

In silico comparison between the mutated and wild-type androgen receptors and their influence on the selection of optimum androgenic receptor blockers for the treatment of prostate cancer [version 4; peer review: 2 approved]

F1000Research
Background: Prostate cancer is a disease that occurs in men aged more than 50 years. In Iraq, 8.89 men per 100,000 population suffer from prostate cancer, with the incidence being 14,016 cases and mortality being 6,367 cases.
Hany Akeel Al-Hussaniy, Mohammed J. AL-Zobaidy, Zahraa S. Al-tameemi   +2 more
doaj   +1 more source