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Ref Type Journal Article
PMID (27274052)
Authors Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H, Siu K, Winkler JD, Crew AP, Crews CM, Coleman KG
Title PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Journal Proceedings of the National Academy of Sciences of the United States of America
Vol 113
Issue 26
Date 2016 06 28
Abstract Text Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States. Although androgen deprivation can initially lead to remission, the disease often progresses to castration-resistant prostate cancer (CRPC), which is still reliant on androgen receptor (AR) signaling and is associated with a poor prognosis. Some success against CRPC has been achieved by drugs that target AR signaling, but secondary resistance invariably emerges, and new therapies are urgently needed. Recently, inhibitors of bromodomain and extra-terminal (BET) family proteins have shown growth-inhibitory activity in preclinical models of CRPC. Here, we demonstrate that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. Unlike BET inhibitors, ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model. This study is, to our knowledge, the first to demonstrate efficacy with a small-molecule BET degrader in a solid-tumor malignancy and potentially represents an important therapeutic advance in the treatment of CRPC.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
ARV-771 ARV 771|ARV771 ARV-771 is a bifunctional molecule that targets BET proteins for proteolytic degradation, resulting in reduced target gene expression and potentially leading to increased apoptosis and reduced tumor growth (PMID: 31217338, PMID: 27274052).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown prostate cancer not applicable ARV-771 Preclinical - Cell line xenograft Actionable In a preclinical study, ARV-771 treatment induced apoptosis and inhibited proliferation of prostate cancer cell lines in culture, and inhibited tumor growth and induced regression in a cell line xenograft model (PMID: 27274052). 27274052
Unknown unknown prostate cancer not applicable Birabresib Preclinical - Cell line xenograft Actionable In a preclinical study, Birabresib (OTX015) treatment inhibited tumor growth in a cell line xenograft model of prostate cancer (PMID: 27274052). 27274052