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Advanced Functional Materials, EarlyView.Schematic illustration of the engineered RN@FDT for multimodal tumor therapy. a) Fabrication of FD&DOX/TFA‐loaded RGD‐NNV (RN@FDT) and the light‐triggered disassemble of RN@FDT. b) After internalized by tumor cells, RN@FDT are disintegrated under NIR‐II laser irradiation to boost PTT and induce cell apoptosis.
Jiahui Zhang +16 more
wiley +1 more source
SRX3177, a CDK4/6-PI3K-BET inhibitor, in combination with an RdRp inhibitor, Molnupiravir, or an entry inhibitor MU-UNMC-2, has potent antiviral activity against the Omicron variant of SARS-CoV-2. [PDF]
Antiviral ResPandey K +8 more
europepmc +1 more source
Physachenolide C is a Potent, Selective BET Inhibitor
Journal of Medicinal Chemistry, 2022 A pulldown using a biotinylated natural product of interest in the 17β-hydroxywithanolide (17-BHW) class, physachenolide C (PCC), identified the bromodomain and extra-terminal domain (BET) family of proteins (BRD2, BRD3, and BRD4), readers of acetyl-lysine modifications and regulators of gene transcription, as potential cellular targets.
Christopher J. Zerio +13 more
core +4 more sources
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Current Opinion in Chemical Biology, 2022
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P. Schwalm, Stefan Knapp
openaire +2 more sources
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P. Schwalm, Stefan Knapp
openaire +2 more sources
Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinoma
International Journal of Cancer, 2020 Pancreatic ductal adenocarcinoma (PDAC) is resistant to virtually all chemo‐ and targeted therapeutic approaches. Epigenetic regulators represent a novel class of drug targets.
Stefan Knapp +2 more
exaly +3 more sources
BET bromodomain inhibitors in leukemia
Experimental Hematology, 2015The last few years have seen the identification of bromodomain and extraterminal (BET) proteins as critical mediators of transcription with effects on its direct control and cisregulation. This discovery is important in furthering our understanding of the mechanisms of normal transcriptional control. Subsequent work has shed light on the multiple roles
Faisal, Basheer, Brian J P, Huntly
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Development of methyl isoxazoleazepines as inhibitors of BET
Bioorganic & Medicinal Chemistry Letters, 2015In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified by carboxamide 23. The methyl isoxazoleazepine chemotype provides potent inhibition of the bromodomains of the BET family ...
Michael C, Hewitt +22 more
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BET bromodomain inhibitors: a patent review
Expert Opinion on Therapeutic Patents, 2013The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT). These "epigenetic readers" bind to acetyllysine (KAc) residues on the tails of histones H3 and H4, and regulate chromatin structure and gene expression.
Jean-Marc, Garnier +2 more
openaire +2 more sources