ArticleInternational journal of molecular sciences2021
Development of Novel Inhibitors Targeting the D-Box of the DNA Binding Domain of Androgen Receptor.
Article in International journal of molecular sciences, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Breaking the bonds: targeting protein dimerization for prostate cancer therapy.Endocrinology · 2026Review
- Splicing factor TRA2B enhances synthesis of androgen receptor variant AR-V7 in prostate cancer cells.The Journal of clinical investigation · 2026Article
- Androgen Receptor Point Mutations: A Mechanism of Therapeutic Resistance and a Framework for Rational Drug Design.Cancers · 2026Review
- Emerging Therapeutic Approaches to Engage the Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.Cancers · 2025Review
- Androgen receptor inhibitors in treating prostate cancer.Asian journal of andrology · 2025Review
- Defining Splicing Factor Requirements for Androgen Receptor Variant Synthesis in Advanced Prostate Cancer.Molecular cancer research : MCR · 2024Article
- Discovery of Novel Anti-Resistance AR Antagonists Guided by Funnel Metadynamics Simulation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Article
- The catalytic subunit of DNA-PK regulates transcription and splicing of AR in advanced prostate cancer.The Journal of clinical investigation · 2023Article
- BRCA-deficient metastatic prostate cancer has an adverse prognosis and distinct genomic phenotype.EBioMedicine · 2023Article
- The Small Molecule Antagonist KCI807 Disrupts Association of the Amino-Terminal Domain of the Androgen Receptor with ELK1 by Modulating the Adjacent DNA Binding Domain.Molecular pharmacology · 2023Article
- Cheminformatic Analysis and Machine Learning Modeling to Investigate Androgen Receptor Antagonists to Combat Prostate Cancer.ACS omega · 2023Article
- Structure-Based Study to Overcome Cross-Reactivity of Novel Androgen Receptor Inhibitors.Cells · 2022Article
- Second generation androgen receptor antagonists and challenges in prostate cancer treatment.Cell death & disease · 2022Review
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Authors and funding
8 authors.
Funding
Abstract
The inhibition of the androgen receptor (AR) is an established strategy in prostate cancer (PCa) treatment until drug resistance develops either through mutations in the ligand-binding domain (LBD) portion of the receptor or its deletion. We previously identified a druggable pocket on the DNA binding domain (DBD) dimerization surface of the AR and reported several potent inhibitors that effectively disrupted DBD-DBD interactions and consequently demonstrated certain antineoplastic activity. Here we describe further development of small molecule inhibitors of AR DBD dimerization and provide their broad biological characterization. The developed compounds demonstrate improved activity in the mammalian two-hybrid assay, enhanced inhibition of AR-V7 transcriptional activity, and improved microsomal stability. These findings position us for the development of AR inhibitors with entirely novel mechanisms of action that would bypass most forms of PCa treatment resistance, including the truncation of the LBD of the AR.
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