Results 1 to 10 of about 17,474 (137)

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

Molecules, 2022
Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities.
Longjun Ma, Yan Zhou, Dehua Yang, Ming-Wei Wang, Wei Lu, Jiyu Jin   +5 more
doaj   +4 more sources

CREB5 Promotes Resistance to Androgen-Receptor Antagonists and Androgen Deprivation in Prostate Cancer [PDF]

Cell Reports, 2019
Summary: Androgen-receptor (AR) inhibitors, including enzalutamide, are used for treatment of all metastatic castration-resistant prostate cancers (mCRPCs). However, some patients develop resistance or never respond. We find that the transcription factor
Justin H. Hwang, Ji-Heui Seo, Michael L. Beshiri, Stephanie Wankowicz, David Liu, Alexander Cheung, Ji Li, Xintao Qiu, Andrew L. Hong, Ginevra Botta, Lior Golumb, Camden Richter, Jonathan So, Gabriel J. Sandoval, Andrew O. Giacomelli, Seav Huong Ly, Celine Han, Chao Dai, Hubert Pakula, Anjali Sheahan, Federica Piccioni, Ole Gjoerup, Massimo Loda, Adam G. Sowalsky, Leigh Ellis, Henry Long, David E. Root, Kathleen Kelly, Eliezer M. Van Allen, Matthew L. Freedman, Atish D. Choudhury, William C. Hahn   +31 more
doaj   +5 more sources

Virtual Screening and Bioactivity Evaluation of Novel Androgen Receptor Antagonists From Anti-PCa Traditional Chinese Medicine Prescriptions [PDF]

Frontiers in Chemistry, 2020
Prostate cancer (PCa), a type of malignancy that arises in the prostate gland, is the most commonly diagnosed neoplasm and the second leading cause of cancer-related deaths in men.
Wenya Han, Yuqi Shi, Jie Su, Zhennan Zhao, Xin Wang, Jiazhong Li, Huanxiang Liu   +6 more
doaj   +2 more sources

Second generation androgen receptor antagonists and challenges in prostate cancer treatment [PDF]

Cell Death and Disease, 2022
Prostate cancer is a hormone-dependent malignancy, whose onset and progression are closely related to the activity of the androgen receptor (AR) signaling pathway.
Yanhua Chen, Qianqian Zhou, William Hankey, Xiaosheng Fang, Fuwen Yuan   +4 more
doaj   +2 more sources

Identifying androgen receptor antagonists using a metabolically competent high-throughput screening assay [PDF]

Current Research in Toxicology
Androgen receptor (AR) is a nuclear receptor with a well-established role in sexual function and development. Modifications in AR can lead to endocrine disruption, cancer, and other diseases, making it imperative to identify compounds that influence ...
Caitlin Lynch, Pranav Shah, Jinghua Zhao, Xin Xu, Ruili Huang, Menghang Xia   +5 more
doaj   +2 more sources

Discovery and Identification of Pyrazolopyramidine Analogs as Novel Potent Androgen Receptor Antagonists [PDF]

Frontiers in Pharmacology, 2018
Androgen receptor (AR), an important target in the current androgen derivation therapy, plays a critical role in the development and progress of prostate cancer (PCa).
Lingyan Wang, Tianqing Song, Xin Wang, Jiazhong Li   +3 more
doaj   +2 more sources

Screening for insulin-independent pathways that modulate glucose homeostasis identifies androgen receptor antagonists [PDF]

eLife, 2018
Pathways modulating glucose homeostasis independently of insulin would open new avenues to combat insulin resistance and diabetes. Here, we report the establishment, characterization, and use of a vertebrate ‘insulin-free’ model to identify insulin ...
Sri Teja Mullapudi, Christian SM Helker, Giulia LM Boezio, Hans-Martin Maischein, Anna M Sokol, Stefan Guenther, Hiroki Matsuda, Stefan Kubicek, Johannes Graumann, Yu Hsuan Carol Yang, Didier YR Stainier   +10 more
doaj   +2 more sources

The protein composition of exosomes released by prostate cancer cells is distinctly regulated by androgen receptor-antagonists and -agonist to stimulate growth of target cells [PDF]

Cell Communication and Signaling
Background Prostate cancer (PCa) is a prevalent malignancy in men worldwide, ranking as the second leading cause of cancer-related death in Western countries. Various PCa hormone therapies, such as androgen receptor (AR)-antagonists or supraphysiological
Golnaz Atri Roozbahani, Miriam Kokal-Ribaudo, Mehdi Heidari Horestani, Thanakorn Pungsrinont, Aria Baniahmad   +4 more
doaj   +2 more sources

Androgen receptor antagonists in castration-resistant prostate cancer. [PDF]

Cancer J, 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 ...
Rathkopf D, Scher HI.
europepmc   +4 more sources

Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Prostate cancer (PCa) is the second leading cause of death in men. Apart from androgen receptor, 5α-reductase has also been recognized as a potential target.
Kejing Lao, Guoliang Xun, Xingchun Gou, Hua Xiang   +3 more
doaj   +2 more sources