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BET mechanisms in cancer

Authors :
Panagis Filippakopoulos
Elizabeth Henderson
Publication Year :
2020
Publisher :
Elsevier, 2020.

Abstract

Bromodomain and extra-terminal (BET) proteins orchestrate a multitude of transcriptional networks through their interactions with acetylated and nonacetylated binding partners. Their association with chromatin dictates important roles in development and cellular homeostasis in normal tissue. However, there is evidence showing their contribution to malignant phenotypes; combined with proof of principle already established for targeting these transcriptional coregulators, there is a strong rationale for the attenuation of their function in cancer. When BET bromodomains are targeted in cells, there are a myriad of responses between and within malignancies. While many of the responses overlap between cancers of varying origins, there are many inconsistencies. Equally, the mechanisms underpinning these downstream events have been uncovered with varying degrees of clarity. Here we highlight those that are common between malignancies, as well as determinants of responses to BET inhibitors. Lastly, there are several limitations to BET inhibitor use, and strategies to circumvent these problems will be discussed.

Details

Database :
OpenAIRE
Accession number :
edsair.doi...........cad1ca39b998143dc711d1e58fd31e22
Full Text :
https://doi.org/10.1016/b978-0-12-816422-8.00006-4