Results 21 to 30 of about 19,533 (266)

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

Androgen Receptor Antagonists in Castration-Resistant Prostate Cancer [PDF]

The Cancer Journal, 2013
Persistent androgen receptor (AR) signaling despite low levels of serum androgens has been identified as a critical target for drug discovery in castration-resistant prostate cancer (CRPC). As proof of principle that the AR remains relevant in CRPC, 2 AR-targeted agents recently approved by the Food and Drug Administration-abiraterone and enzalutamide ...
Dana, Rathkopf, Howard I, Scher
openaire   +2 more sources

The characteristics of adverse reactions of three anti-prostate cancer drugs based on Vigiaccess database and bibliometric analysis

Frontiers in Pharmacology
BackgroundAndrogen antagonists, including apalutamide, darolutamide, and enzalutamide, play a crucial role in the treatment of prostate cancer.
Jianqing Wang, Jia You, Weixing Huang, Weixing Huang, Chiting Yuan, Jiangjie Chen, Feifei Wang, Wei Wang, Liwei Zhang, Liwei Zhang   +9 more
doaj   +1 more source

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

Androgen deprivation therapy and side effects: are GnRH antagonists safer?

Asian Journal of Andrology, 2021
Androgen deprivation therapy (ADT) with gonadotropin-releasing hormone (GnRH) agonists and antagonists is the mainstay of advanced prostate cancer treatment. Both drug classes decrease levels of luteinizing hormone and follicle-stimulating hormones (FSH),
Stephen J Freedland, Per-Anders Abrahamsson   +1 more
doaj   +1 more source

Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

Molecules, 2022
Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide.
Longjun Ma, Yan Zhou, Dehua Yang, Ming-Wei Wang, Wei Lu, Jiyu Jin   +5 more
openaire   +3 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

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

Bidirectional Synaptic Plasticity Is Driven by Sex Neurosteroids Targeting Estrogen and Androgen Receptors in Hippocampal CA1 Pyramidal Neurons

Frontiers in Cellular Neuroscience, 2019
Neuroactive estrogenic and androgenic steroids influence synaptic transmission, finely modulating synaptic plasticity in several brain regions including the hippocampus.
Alessandro Tozzi, Valentina Durante, Paolo Manca, Michela Di Mauro, Juan Blasi, Silvarosa Grassi, Paolo Calabresi, Suguru Kawato, Suguru Kawato, Vito Enrico Pettorossi   +9 more
doaj   +1 more source

PARP inhibition and pharmacological ascorbate demonstrate synergy in castration‐resistant prostate cancer

Molecular Oncology, EarlyView.
Pharmacologic ascorbate (vitamin C) increases ROS, disrupts cellular metabolism, and induces DNA damage in CRPC cells. These effects sensitize tumors to PARP inhibition, producing synergistic growth suppression with olaparib in vitro and significantly delayed tumor progression in vivo. Pyruvate rescue confirms ROS‐dependent activity.
Nicolas Gordon, Peter T. Gallagher, Orly I. Richter, Neermala Poudel Neupane, Amy C. Mandigo, Jennifer J. McCann, Emanuela Dylgjeri, Irina Vasilevskaya, Christopher McNair, Channing J. Paller, Wm. Kevin Kelly, Karen E. Knudsen, Matthew J. Schiewer, Ayesha A. Shafi   +13 more
wiley   +1 more source