ArticleScientific reports2018
Determining direct binders of the Androgen Receptor using a high-throughput Cellular Thermal Shift Assay.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed.
- A non-canonical androgen signaling pathway drives microglial activation and tau pathology in females.Research square · 2026Article
- SC912 inhibits AR-V7 activity in castration-resistant prostate cancer by targeting the androgen receptor N-terminal domain.Oncogene · 2024Article
- Deep learning based CETSA feature prediction cross multiple cell lines with latent space representation.Scientific reports · 2024Article
- Characterization of allosteric modulators that disrupt androgen receptor co-activator protein-protein interactions to alter transactivation-Drug leads for metastatic castration resistant prostate cancer.SLAS discovery : advancing life sciences R & D · 2023Article
- Thermal unfolding methods in drug discovery.Biophysics reviews · 2023Review
- A Shift in Thinking: Cellular Thermal Shift Assay-Enabled Drug Discovery.ACS medicinal chemistry letters · 2023Review
- Comparative Proteomic and Transcriptomic Analysis of the Impact of Androgen Stimulation and Darolutamide Inhibition.Cancers · 2022Article
- Current and emerging target identification methods for novel antimalarials.International journal for parasitology. Drugs and drug resistance · 2022Review
- Alkaloid Derivative (Molecules (Basel, Switzerland) · 2022Article
- Real-Time Cellular Thermal Shift Assay to Monitor Target Engagement.ACS chemical biology · 2022Article
- High intratumoral dihydrotestosterone is associated with antiandrogen resistance in VCaP prostate cancer xenografts in castrated mice.iScience · 2022Article
- Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry.Molecules (Basel, Switzerland) · 2021Review
- TAK1/AP-1-Targeted Anti-Inflammatory Effects ofMolecules (Basel, Switzerland) · 2021Article
- Article
- Regulation and targeting of androgen receptor nuclear localization in castration-resistant prostate cancer.The Journal of clinical investigation · 2021Article
- A property-response perspective on modern toxicity assessment and drug toxicity index (DTI).In silico pharmacology · 2021Review
- Indirect Detection of Ligand Binding by Thermal Melt Analysis.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Importance of Quantifying Drug-Target Engagement in Cells.ACS medicinal chemistry letters · 2020Article
- 3-Deoxy-2β,16-dihydroxynagilactone E, a natural compound from Podocarpus nagi, preferentially inhibits JAK2/STAT3 signaling by allosterically interacting with the regulatory domain of JAK2 and induces apoptosis of cancer cells.Acta pharmacologica Sinica · 2019Article
- Androgenic Effects on Ventricular Repolarization: A Translational Study From the International Pharmacovigilance Database to iPSC-Cardiomyocytes.Circulation · 2019Article
Corrections and comments
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Androgen Receptor (AR) is a key driver in prostate cancer. Direct targeting of AR has valuable therapeutic potential. However, the lack of disease relevant cellular methodologies capable of discriminating between inhibitors that directly bind AR and those that instead act on AR co-regulators has made identification of novel antagonists challenging. The Cellular Thermal Shift Assay (CETSA) is a technology enabling confirmation of direct target engagement with label-free, endogenous protein in living cells. We report the development of the first high-throughput CETSA assay (CETSA HT) to identify direct AR binders in a prostate cancer cell line endogenously expressing AR. Using this approach, we screened a pharmacology library containing both compounds reported to directly engage AR, and compounds expected to target AR co-regulators. Our results show that CETSA HT exclusively identifies direct AR binders, differentiating them from co-regulator inhibitors where other cellular assays measuring functional responses cannot. Using this CETSA HT approach we can derive apparent binding affinities for a range of AR antagonists, which represent an intracellular measure of antagonist-receptor Ki performed for the first time in a label-free, disease-relevant context. These results highlight the potential of CETSA HT to improve the success rates for novel therapeutic interventions directly targeting AR.
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