What is it about?
Small cell lung cancer (SCLC) has a dismal prognosis due to it's rapid growth and resistance to chemotherapy. Proliferation and differentiation of SCLC is controlled by protein members of the oncogenic MYC. Inhibition or degradation of MYC is difficult but can be indirectly achieved by inhibitors directed to bromodomain proteins (BET). In particular, Proteolysis Targeting Chimeras (PROTACs) directed at BRD4 or other members of the BET-family impair the expression of MYC and inhibit proliferation of SCLC cells. First PROTACs directed at hormone receptors are in clinical trials and this class of agents will become a regular part of precision medicine therapies.
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Why is it important?
This is the first time that BET-directed PROTACs have been shown to reduce the proliferation of SCLC cell lines by the indirect effects of these agents on the expression of MYC that is otherwise difficult to target.
Perspectives
PROTACs and especially PROTACs directed at bromodomain proteins will become an important tool in the treatment of cancer patients.
Sandra Stickler
Medical University of Vienna
Read the Original
This page is a summary of: Bromodomain Protein-directed Agents and MYC in Small Cell Lung
Cancer, Current Cancer Drug Targets, September 2024, Bentham Science Publishers,
DOI: 10.2174/0115680096272757231211113206.
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