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- Proximity Biosensor Assay for PROTAC Ternary Complex Analysis - ChemRxiv
The assay is applied to cereblon (CRBN) and von Hippel-Lindau (VHL) as E3 ligase substrate receptors, a range of compounds including AT1, MZ1, dBETs, and ARV-825 as PROTACs, and the two bromodomains of Brd2, Brd3, Brd4, and BrdT proteins as targets
- A comprehensive review of BET-targeting PROTACs for cancer therapy
Consistent with its potent and prolonged BRD4 and c-Myc depletion effects, ARV-825 exhibited superior antiproliferative and apoptotic activity against Burkitt’s lymphoma cells when compared with those of BRD4 inhibitors
- Current strategies for the design of PROTAC linkers: a critical review
This “macro-PROTAC” (94) exhibited positive cooperativity in formation of TC with BD2 of BRD2-4 (α = 9 5, 4 0, and 10 5 for BRD2, BRD3 and BRD4 respectively), but no cooperativity with BD1 (α < 1 in all cases), suggesting better differentiation between the two bromodomains than its parent MZ1 (1)
- Nanoformulation of BRD4-Degrading PROTAC: Improving Druggability To . . .
In a recent study, Saraswat and colleagues identified a novel proteolysis targeting chimera (PROTAC), ARV-825 (ARV), that efficiently degrades bromodomain-containing protein 4 (BRD4) to drug the ‘undruggable’ MYC in pancreatic cancer
- The BET inhibitor degrader ARV-825 prolongs the growth arrest response . . .
In contrast to the relative lack of impact of autophagy inhibition, the BET degrader, ARV-825, significantly prolonged growth arrest and delayed proliferative recovery in both p53 wildtype MCF-7 cells and p53 mutant T-47D cells independent of Rb status
- ARV-825 | 99. 45%(HPLC) | In Stock | PROTAC chemical - Selleckchem. com
ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC
- BRD4 Proteolysis Targeting Chimera (PROTAC) ARV-825 Targets Both NOTCH1 . . .
ARV-825 recruits BRD4 to the E3 ubiquitin ligase cereblon and leads to efficient and sustained degradation of BRD4, resulting in down-regulation of MYC Methods: We investigated the effectiveness of ARV-825 against T-ALL cell lines, including GSI-resistant lines
- ARV-825-induced BRD4 protein degradation as a therapy for . . . - PubMed
BRD4 protein degradation as well as c-Myc, Bcl-xL and cyclin D1 downregulation were detected in ARV-825-treated TPC-1 tumor tissues Taken together, ARV-825 induces BRD4 protein degradation and inhibits thyroid carcinoma cell growth in vitro and in vivo
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