ArticleNature communications2013
Peptidomimetic targeting of critical androgen receptor-coregulator interactions in prostate cancer.
Article in Nature communications, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 74 papers.
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Who cites it
74 citing papers in PubMed, 256 citations in OpenAlex.
- The PELP1 Pathway and Its Importance in Cancer Treatment.Biomolecules · 2025Review
- Evolving roles for the androgen receptor and its protein interactome in castration-resistant prostate cancer.Oncogene · 2025Review
- Disrupting the interaction between androgen receptor and its coregulator WDR77 delays the growth of treatment-resistant prostate cancer.Cell reports · 2025Article
- From Concepts to Inhibitors: A Blueprint for Targeting Protein-Protein Interactions.Chemical reviews · 2025Review
- Development of cyclopeptide inhibitors specifically disrupting FXR-coactivator interaction in the intestine as a novel therapeutic strategy for MASH.Life metabolism · 2025Article
- Structure-Activity Relationship Study of Tris-Benzamides as Estrogen Receptor Coregulator Binding Modulators.ACS pharmacology & translational science · 2024Article
- International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023.Pharmacological reviews · 2023Review
- Tetrasubstituted Pyrrole Derivative Mimetics of Protein-Protein Interaction Hot-Spot Residues: A Promising Class of Anticancer Agents Targeting Melanoma Cells.Molecules (Basel, Switzerland) · 2023Article
- Targeting LIPA independent of its lipase activity is a therapeutic strategy in solid tumors via induction of endoplasmic reticulum stress.Nature cancer · 2022Article
- Harnessing the Heterogeneity of Prostate Cancer for Target Discovery Using Patient-Derived Explants.Cancers · 2022Article
- Analyzing the Androgen Receptor Interactome in Prostate Cancer: Implications for Therapeutic Intervention.Cells · 2022Review
- The central role of Sphingosine kinase 1 in the development of neuroendocrine prostate cancer (NEPC): A new targeted therapy of NEPC.Clinical and translational medicine · 2022Article
- From Therapy Resistance to Targeted Therapies in Prostate Cancer.Frontiers in oncology · 2022Review
- AR Structural Variants and Prostate Cancer.Advances in experimental medicine and biology · 2022Article
- IFN-γ activates the tumor cell-intrinsic STING pathway through the induction of DNA damage and cytosolic dsDNA formation.Oncoimmunology · 2022Article
- Neurodegenerative Disease: Roles for Sex, Hormones, and Oxidative Stress.Endocrinology · 2021Review
- PELP1/SRC-3-dependent regulation of metabolic PFKFB kinases drives therapy resistant EROncogene · 2021Article
- Query-guided protein-protein interaction inhibitor discovery.Chemical science · 2021Article
- Dynamic differences between DNA damage repair responses in primary tumors and cell lines.Translational oncology · 2021Article
- IFN-γ-induced ER stress impairs autophagy and triggers apoptosis in lung cancer cells.Oncoimmunology · 2021Article
14 more citing papers are in PubMed but not listed here.
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Authors and funding
9 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The growth of advanced prostate cancer depends on androgen receptor signalling, however treatment options are limited. Here we report the disruption of specific protein-protein interactions involving LXXLL motifs in androgen receptor-coregulator proteins such as PELP1 using a novel, small molecule peptidomimetic (D2). D2 is stable, non-toxic and efficiently taken up by prostate cancer cells. Importantly, D2 blocks androgen-induced nuclear uptake and genomic activity of the androgen receptor. Furthermore, D2 abrogates androgen-induced proliferation of prostate cancer cells in vitro with an IC50 of 40 nM, and inhibits tumour growth in a mouse xenograft model. D2 also disrupts androgen receptor-coregulator interactions in ex vivo cultures of primary human prostate tumours. These findings provide evidence that targeting androgen receptor-coregulator interactions using peptidomimetics may be a viable therapeutic approach for patients with advanced prostate cancer.
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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.