BET proteins as targets for anticancer treatment

A Stathis, F Bertoni - Cancer discovery, 2018 - AACR
Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …

[HTML][HTML] The mechanisms behind the therapeutic activity of BET bromodomain inhibition

J Shi, CR Vakoc - Molecular cell, 2014 - cell.com
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …

Discovery of a small-molecule degrader of bromodomain and extra-terminal (BET) proteins with picomolar cellular potencies and capable of achieving tumor …

B Zhou, J Hu, F Xu, Z Chen, L Bai… - Journal of medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3,
BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in …

Discovery of QCA570 as an exceptionally potent and efficacious proteolysis targeting chimera (PROTAC) degrader of the bromodomain and extra-terminal (BET) …

C Qin, Y Hu, B Zhou, E Fernandez-Salas… - Journal of medicinal …, 2018 - ACS Publications
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and
promising therapeutic targets for cancer and other human diseases. We describe herein a …

[HTML][HTML] Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

[HTML][HTML] Ex vivo analysis identifies effective HIV-1 latency–reversing drug combinations

GM Laird, CK Bullen, DIS Rosenbloom… - The Journal of …, 2015 - Am Soc Clin Investig
Reversal of HIV-1 latency by small molecules is a potential cure strategy. This approach will
likely require effective drug combinations to achieve high levels of latency reversal. Using …

New ex vivo approaches distinguish effective and ineffective single agents for reversing HIV-1 latency in vivo

CK Bullen, GM Laird, CM Durand, JD Siliciano… - Nature medicine, 2014 - nature.com
HIV-1 persists in a latent reservoir despite antiretroviral therapy (ART),,,,. This reservoir is the
major barrier to HIV-1 eradication,. Current approaches to purging the latent reservoir …

Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …

[HTML][HTML] The current status of latency reversing agents for HIV-1 remission

A Rodari, G Darcis, CM Van Lint - Annual review of virology, 2021 - annualreviews.org
Combinatory antiretroviral therapy (cART) reduces human immunodeficiency virus type 1
(HIV-1) replication but is not curative because cART interruption almost invariably leads to a …

[HTML][HTML] BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia

W Kong, A Dimitri, W Wang, IY Jung… - The Journal of …, 2021 - Am Soc Clin Investig
Chimeric antigen receptor (CAR) T cells have induced remarkable antitumor responses in B
cell malignancies. Some patients do not respond because of T cell deficiencies that hamper …