ArticleMolecular cancer therapeutics2013
AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo.
Article in Molecular cancer therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 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
38 citing papers in PubMed, 77 citations in OpenAlex.
- Targeting the Androgen Receptor and Associated Cofactors in Prostate Cancer: Novel Approaches and Future Perspectives.International journal of molecular sciences · 2026Review
- Hydrophobic tagging: A promising paradigm for targeted protein degradation.Cell insight · 2026Review
- Androgen receptor signalling in non-prostatic malignancies: challenges and opportunities.Nature reviews. Cancer · 2025Review
- Nuclear lamin A/C phosphorylation by loss of androgen receptor leads to cancer-associated fibroblast activation.Nature communications · 2024Article
- Androgen drives melanoma invasiveness and metastatic spread by inducing tumorigenic fucosylation.Nature communications · 2024Article
- Recent advances in targeted protein degraders as potential therapeutic agents.Molecular diversity · 2024Review
- Targeted Investigational Oncology Agents in the NCI-60: A Phenotypic Systems-based Resource.Molecular cancer therapeutics · 2023Article
- Androgen receptor is a determinant of melanoma targeted drug resistance.Nature communications · 2023Article
- Review
- Lysine Acetyltransferases and Their Role in AR Signaling and Prostate Cancer.Frontiers in endocrinology · 2022Review
- Review
- Sustained androgen receptor signaling is a determinant of melanoma cell growth potential and tumorigenesis.The Journal of experimental medicine · 2021Article
- Eighty Years of Targeting Androgen Receptor Activity in Prostate Cancer: The Fight Goes on.Cancers · 2021Review
- Current Biomarkers for Precision Medicine in Breast Cancer.Advances in experimental medicine and biology · 2021Article
- Bromodomain and BET family proteins as epigenetic targets in cancer therapy: their degradation, present drugs, and possible PROTACs.RSC advances · 2020Review
- Alzheimer's Disease, and Breast and Prostate Cancer Research: Translational Failures and the Importance to Monitor Outputs and Impact of Funded Research.Animals : an open access journal from MDPI · 2020Review
- Therapies Targeted to Androgen Receptor Signaling Axis in Prostate Cancer: Progress, Challenges, and Hope.Cancers · 2019Review
- Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.ACS medicinal chemistry letters · 2019Article
- Androgen Receptor-Directed Molecular Conjugates for Targeting Prostate Cancer.Frontiers in chemistry · 2019Review
- Targeting Brd4 for cancer therapy: inhibitors and degraders.MedChemComm · 2018Review
Corrections and comments
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Authors and funding
25 authors at 2 institutions in 1 country.
Funding
Abstract
Continued androgen receptor (AR) expression and signaling is a key driver in castration-resistant prostate cancer (CRPC) after classical androgen ablation therapies have failed, and therefore remains a target for the treatment of progressive disease. Here, we describe the biological characterization of AZD3514, an orally bioavailable drug that inhibits androgen-dependent and -independent AR signaling. AZD3514 modulates AR signaling through two distinct mechanisms, an inhibition of ligand-driven nuclear translocation of AR and a downregulation of receptor levels, both of which were observed in vitro and in vivo. AZD3514 inhibited testosterone-driven seminal vesicle development in juvenile male rats and the growth of androgen-dependent Dunning R3327H prostate tumors in adult rats. Furthermore, this class of compound showed antitumor activity in the HID28 mouse model of CRPC in vivo. AZD3514 is currently in phase I clinical evaluation.
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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.