ReviewFrontiers in pharmacology2015
Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance.
Review in Frontiers in pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 16 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 31 citations in OpenAlex.
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- Impact of STAT Proteins in Tumor Progress and Therapy Resistance in Advanced and Metastasized Prostate Cancer.Cancers · 2021Review
- PARP7 mono-ADP-ribosylates the agonist conformation of the androgen receptor in the nucleus.The Biochemical journal · 2021Article
- Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry · 2021Article
- Selective targeting of the androgen receptor-DNA binding domain by the novel antiandrogen SBF-1 and inhibition of the growth of prostate cancer cells.Investigational new drugs · 2021Article
- Review
- Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.Journal of medicinal chemistry · 2020Article
- re-TAMD: exploring interactions between H3 peptide and YEATS domain using enhanced sampling.BMC structural biology · 2018Article
- Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer.ACS medicinal chemistry letters · 2018Article
- Inhibition of Androgen Receptor Function and Level in Castration-Resistant Prostate Cancer Cells by 2-[(isoxazol-4-ylmethyl)thio]-1-(4-phenylpiperazin-1-yl)ethanone.Endocrinology · 2017Article
- Inhibition of Androgen Receptor Nuclear Localization and Castration-Resistant Prostate Tumor Growth by Pyrroloimidazole-based Small Molecules.Molecular cancer therapeutics · 2017Article
- 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment.Journal of medicinal chemistry · 2017Article
- Silencing the roadblocks to effective triple-negative breast cancer treatments by siRNA nanoparticles.Endocrine-related cancer · 2017Review
- Identification of Triptophenolide fromACS medicinal chemistry letters · 2016Article
- The hunt for a selective 17,20 lyase inhibitor; learning lessons from nature.The Journal of steroid biochemistry and molecular biology · 2016Review
- Article
Corrections and comments
- Erratum issued
Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Androgen receptor (AR) plays a critical role in the development and progression of prostate cancer (PCa). Current clinically used antiandrogens such as flutamide, bicalutamide, and newly approved enzalutamide mainly target the hormone binding pocket (HBP) of AR. However, over time, drug resistance invariably develops and switches these antiandrogens from antagonist to agonist of the AR. Accumulated evidence indicates that AR mutation is an important cause for the drug resistance. This review will give an overview of the mutation based resistance of the current clinically used antiandrogens and the rational drug design to overcome the resistance, provides a promising strategy for the development of the new generation of antiandrogens targeting HBP.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.