PROTAC induced-BET protein degradation exhibits potent anti
Oct 25, 2019 · In this study, we investigated the in vitro and in vivo anti-osteosarcoma activity by targeting BET with a PROTAC molecule BETd-260. The results showed that BETd-260 …
PROTAC-induced BET protein degradation as a therapy for …
Jun 28, 2016 · Here, we demonstrate that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved …
A comprehensive review of BET-targeting PROTACs for cancer …
Nov 1, 2022 · Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) has emerged as an effective strategy for drug discovery, given their unique advantages over target …
Targeting BET Proteins With a PROTAC Molecule Elicits Potent …
BET proteins have been found to be overexpressed in HCC cells and tumor tissues. However, the biological activity of BET-PROTACs in hepatocellular carcinoma (HCC) remains unclear. In …
Acquired Resistance to BET-PROTACs (Proteolysis-Targeting …
Using BET-PROTACs as a model system, we demonstrate that resistance to both VHL- and CRBN-based PROTACs can occur in cancer cells following chronic treatment. However, …
BET protein proteolysis targeting chimera (PROTAC) exerts
Jun 30, 2017 · Novel BET protein proteolysis targeting chimera (BET-PROTAC) exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm …
Targeting BET Proteins With a PROTAC Molecule Elicits Potent …
Jan 14, 2020 · Targeting BET proteins for degradation using proteolysis-targeting chimera (PROTAC) recently has drawn increasing attention in the field of cancer therapeutics. BET …
Targeted protein degradation reveals BET bromodomains as the …
Jul 1, 2023 · We develop a PROTAC based on Hedgehog Pathway Inhibitor-1 (HPI-1), a phenotypic screen hit with unknown cellular target. Using this Hedgehog Pathway PROTAC …
Novel BET protein Proteolysis Targeting Chimera (BET-PROTAC…
The PROTAC (proteolysis-targeting chimera) ARV-825 recruits bromodomain and extraterminal (BET) proteins to the E3 ubiquitin ligase cereblon, leading to degradation of BET proteins, …
PROTAC induced-BET protein degradation exhibits potent anti ...
Oct 25, 2019 · In this study, we investigated the in vitro and in vivo anti-osteosarcoma activity by targeting BET with a PROTAC molecule BETd-260. The results showed that BETd-260 …