{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["10(11)"],"submitter":["Shi C"],"pubmed_abstract":["Targeting oncogenic proteins for degradation using proteolysis-targeting chimera (PROTAC) recently has drawn increasing attention in the field of cancer research. Bromodomain and extra-terminal (BET) family proteins are newly identified cancer-related epigenetic regulators, which have a role in the pathogenesis and progression of osteosarcoma. 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 completely depletes BET proteins and potently suppresses cell viability in MNNG/HOS, Saos-2, MG-63, and SJSA-1 osteosarcoma cell lines. Compared with BET inhibitors HJB-97 and JQ1, the activity of BETd-260 increased over 1000 times. Moreover, BETd-260 substantially inhibited the expressi"],"journal":["Cell death & disease"],"pagination":["815"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6814818"],"repository":["biostudies-literature"],"pubmed_title":["PROTAC induced-BET protein degradation exhibits potent anti-osteosarcoma activity by triggering apoptosis."],"pmcid":["PMC6814818"],"pubmed_authors":["Wang P","Shi C","Zhang Y","Zhang H","Xu D","Wang H","Zhang S","Yin L","Wang K"],"additional_accession":[]},"is_claimable":false,"name":"PROTAC induced-BET protein degradation exhibits potent anti-osteosarcoma activity by triggering apoptosis.","description":"Targeting oncogenic proteins for degradation using proteolysis-targeting chimera (PROTAC) recently has drawn increasing attention in the field of cancer research. Bromodomain and extra-terminal (BET) family proteins are newly identified cancer-related epigenetic regulators, which have a role in the pathogenesis and progression of osteosarcoma. 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 completely depletes BET proteins and potently suppresses cell viability in MNNG/HOS, Saos-2, MG-63, and SJSA-1 osteosarcoma cell lines. Compared with BET inhibitors HJB-97 and JQ1, the activity of BETd-260 increased over 1000 times. Moreover, BETd-260 substantially inhibited the expressi","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019 Oct","modification":"2025-04-05T13:18:56.624Z","creation":"2019-11-07T08:07:30Z"},"accession":"S-EPMC6814818","cross_references":{"pubmed":["31653826"],"doi":["10.1038/s41419-019-2022-2"]}}