ArticleJournal of medicinal chemistry2012
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 55 citations in OpenAlex.
- Development of cyclopeptide inhibitors specifically disrupting FXR-coactivator interaction in the intestine as a novel therapeutic strategy for MASH.Life metabolism · 2025Article
- Androgen receptor inhibitors in treating prostate cancer.Asian journal of andrology · 2025Review
- DataPype: A Fully Automated Unified Software Platform for Computer-Aided Drug Design.ACS omega · 2023Article
- DeepAR: a novel deep learning-based hybrid framework for the interpretable prediction of androgen receptor antagonists.Journal of cheminformatics · 2023Article
- Discovery of novel antagonists targeting the DNA binding domain of androgen receptor by integrated docking-based virtual screening and bioassays.Acta pharmacologica Sinica · 2022Article
- Allosteric Binding Sites On Nuclear Receptors: Focus On Drug Efficacy and Selectivity.International journal of molecular sciences · 2020Article
- Steroid receptor/coactivator binding inhibitors: An update.Molecular and cellular endocrinology · 2019Review
- A Structure-Activity Relationship Study of Bis-Benzamides as Inhibitors of Androgen Receptor-Coactivator Interaction.Molecules (Basel, Switzerland) · 2019Article
- Structural Based Screening of Antiandrogen Targeting Activation Function-2 Binding Site.Frontiers in pharmacology · 2018Article
- Antagonizing the Androgen Receptor with a Biomimetic Acyltransferase.ACS chemical biology · 2016Article
- Targeting the androgen receptor with steroid conjugates.Journal of medicinal chemistry · 2014Review
- Identification of a New RXRα Antagonist Targeting the Coregulator-Binding Site.ACS medicinal chemistry letters · 2014Article
- Sulindac-derived RXRα modulators inhibit cancer cell growth by binding to a novel site.Chemistry & biology · 2014Article
- (Z)-4-[(2-Amino-4,5-dichloro-anilino)(phenyl)methyl-idene]-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one.Acta crystallographica. Section E, Structure reports online · 2012Article
- {2,2'-[Cyclo-hexane-1,2-diylbis(nitrilo-methanyl-ylidene)]diphenolato}copper(II).Acta crystallographica. Section E, Structure reports online · 2012Article
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Prostate cancer (PCa) therapy typically involves administration of "classical" antiandrogens, competitive inhibitors of androgen receptor (AR) ligands, dihydrotestosterone (DHT) and testosterone (tes), for the ligand-binding pocket (LBP) in the ligand-binding domain (LBD) of AR. Prolonged LBP-targeting leads to resistance, and alternative therapies are urgently required. We report the identification and characterization of a novel series of diarylhydrazides as selective disruptors of AR interaction with coactivators through application of structure and ligand-based virtual screening. Compounds demonstrate full ("true") antagonism in AR with low micromolar potency, selectivity over estrogen receptors α and β and glucocorticoid receptor, and partial antagonism of the progesterone receptor. MDG506 (5) demonstrates low cellular toxicity in PCa models and dose responsive reduction of classical antiandrogen-induced prostate specific antigen expression. These data provide compelling evidence for such non-LBP intervention as an alternative approach or in combination with classical PCa therapy.
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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.