Work

Degradation of BRD4 - a promising treatment approach not only for hematologic but also for solid cancer.

Year: 2021

Type: article

Abstract: 0.5-5 µM). Interestingly, when combined with commonly used cytotoxic therapeutics, dBET6 was found to promote anti-neoplastic effects and to counteract chemoresistance in most cancer cell lines. Moreover, JQ1 and both BET degraders strongly downregulated baseline and interferon-gamma induced expression of the immune checkpoint molecule PD-L1 in all cancer cell lines. Together, our data suggest that dBET6 outperforms first-generation BRD4 targeting drugs like dBET1 and JQ1, and decreases chemoresistance and immune resistance of cancer.

Source: PubMed Central

Authors: Karin Bauer, Anna S Berghoff, Matthias Preusser, Gerwin Heller, Christoph C Zielinski, Peter Valent, Thomas W Grunt

Institutions: Comprehensive Cancer Center Vienna, Ludwig Boltzmann Institute for Hematology and Oncology, Medical University of Vienna

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W3128458146

FWCI: 1.502

Cites: 51

Cited by: 24

Related to: 10