ArticleInternational journal of biological sciences2019
Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib.
Article in International journal of biological sciences, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 29 citations in OpenAlex.
- Emerging Targeted and Multimodal Therapeutic Strategies in Breast Cancer: A Comprehensive Review.Breast cancer (Dove Medical Press) · 2026Review
- AR/ERK co-targeting triggers ferroptosis via FOXC2 in triple-negative breast cancer.Science China. Life sciences · 2026Article
- Editor's Note on 'Inhibition of cyclin D1 expression by androgen receptor in breast cancer cells-identification of a novel androgen response element'.Nucleic acids research · 2025Article
- Using bioinformatics and artificial intelligence to map the cyclin-dependent kinase 4/6 inhibitor biomarker landscape in breast cancer.Future oncology (London, England) · 2024Review
- A deep learning model of tumor cell architecture elucidates response and resistance to CDK4/6 inhibitors.Nature cancer · 2024Article
- The Evolving Pathways of the Efficacy of and Resistance to CDK4/6 Inhibitors in Breast Cancer.Cancers · 2023Review
- Co-targeting RANK pathway treats and prevents acquired resistance to CDK4/6 inhibitors in luminal breast cancer.Cell reports. Medicine · 2023Article
- A narrative review about CDK4/6 inhibitors in the setting of drug resistance: updates on biomarkers and therapeutic strategies in breast cancer.Translational cancer research · 2023Review
- Multimodal perturbation analyses of cyclin-dependent kinases reveal a network of synthetic lethalities associated with cell-cycle regulation and transcriptional regulation.Scientific reports · 2023Article
- CDK4/6 inhibitor resistance mechanisms and treatment strategies (Review).International journal of molecular medicine · 2022Review
- Combination of Cyclin-Dependent Kinase 4 Inhibitors and Androgen Receptor Inhibitors as Cancer Therapy.ACS medicinal chemistry letters · 2022Article
- Cyclin-dependent Kinase 4/6 Inhibitor Palbociclib in Combination with Ralaniten Analogs for the Treatment of Androgen Receptor-positive Prostate and Breast Cancers.Molecular cancer therapeutics · 2022Article
- Diverse role of androgen action in human breast cancer.Endocrine oncology (Bristol, England) · 2022Review
- The Combination of the CDK4/6 Inhibitor, Palbociclib, With the Vitamin DFrontiers in endocrinology · 2022Article
- Intrinsic and acquired resistance to CDK4/6 inhibitors and potential overcoming strategies.Acta pharmacologica Sinica · 2021Review
- Potential Prospect of CDK4/6 Inhibitors in Triple-Negative Breast Cancer.Cancer management and research · 2021Review
- BCL11A confers cell invasion and migration in androgen receptor-positive triple-negative breast cancer.Oncology letters · 2020Article
- Progress: Targeted Therapy, Immunotherapy, and New Chemotherapy Strategies in Advanced Triple-Negative Breast Cancer.Cancer management and research · 2020Review
- Recent advances with cyclin-dependent kinase inhibitors: therapeutic agents for breast cancer and their role in immuno-oncology.Expert review of anticancer therapy · 2019Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The dysregulation of cyclin D -Cyclin-dependent kinase 4/6 (CDK4/6)-Rb axis has been implicated in breast cancer progression and the selective CDK4/6 inhibitors have shown effective activity in advanced breast cancer, especially in tumors driven by the estrogen receptor (ER). However, resistance to these small molecular inhibitors has become an inevitable clinical issue after their initial use. Here, we investigated the potential mechanism of resistance by establishing a CDK4/6 inhibitor palbociclib-resistant breast cancer cell line (MCF-7pR). After prolonged exposure to palbociclib, we detected the loss of the ER signaling and an increase in androgen receptor (AR). Moreover, we demonstrated more localization of AR in the cell nucleus of MCF-7pR compared to the parental cell (MCF-7). We also reported that AR could promote the progression of the cell cycle. Blockade of AR signaling could reduce the level of the relative G1-S cyclins, abolish Rb phosphorylation and inhibit the activation of transcriptional programs in S phase. Furthermore, dual inhibition of AR and CDK4/6 could reverse the resistance of palbociclib both
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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.