Results 11 to 20 of about 767,969 (287)
BET Bromodomain Inhibition Synergizes with PARP Inhibitor in Epithelial Ovarian Cancer [PDF]
Cell Reports, 2017 Summary: PARP inhibition is known to be an effective clinical strategy in BRCA mutant cancers, but PARP inhibition has not been applied to BRCA-proficient tumors.
Sergey Karakashev +11 more
doaj +3 more sources
Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. [PDF]
PLoS ONE, 2016 Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a sequence
Laura Lori +7 more
doaj +5 more sources
, 2019 9th Bet Debora Conference "Jewish Women: Being Present, Bringing Change" covered following topics: contemporary women’s perspectives on Jewish tradition; advocacy for other minority groups: activism against antisemitism, antiziganism, racism, and ...
core +7 more sources
Cells, 2022 Background: Myeloid cells are critical determinants of the sustained inflammation in Crohn’s Disease (CD). Targeting such cells may be an effective therapeutic approach for refractory CD patients. Bromodomain and extra-terminal domain protein inhibitors (
Ahmed M. I. Elfiky +17 more
doaj +1 more source
Bromodomain and Extra-Terminal (BET) Domain Protein Inhibitors for Solid Tumor Cancers [PDF]
Journal of Immunotherapy and Precision Oncology, 2020 The bromodomain and extraterminal (BET) domain protein family is involved in the process of transcription of genetic information. The BET protein family includes BRD2, BRD3, BRD4, and bromodomain testis-specific protein.
Martin V. Nguyen +2 more
doaj +1 more source
Methylpyrrole inhibitors of BET bromodomains [PDF]
Bioorganic & Medicinal Chemistry Letters, 2017 An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments guided by structure-based design provided lead molecules with significant activity in a mouse tumor model. Further modifications to the methylpyrrole core provided compounds with improved properties and enhanced ...
Lisa A, Hasvold +27 more
openaire +2 more sources
BET inhibitor suppresses migration of human hepatocellular carcinoma by inhibiting SMARCA4
Scientific Reports, 2021 Hepatocellular carcinoma (HCC) is one of the most prevalent and poorly responsive cancers worldwide. Bromodomain and extraterminal (BET) inhibitors, such as JQ1 and OTX-015, inhibit BET protein binding to acetylated residues in histones.
Hae In Choi +7 more
doaj +1 more source
Design and characterization of bivalent BET inhibitors [PDF]
Nature Chemical Biology, 2016 Cellular signaling is often propagated by multivalent interactions. Multivalency creates avidity, allowing stable biophysical recognition. Multivalency is an attractive strategy for achieving potent binding to protein targets, as the affinity of bivalent ligands is often greater than the sum of monovalent affinities.
Tanaka, Minoru +8 more
openaire +4 more sources
Neoplasia: An International Journal for Oncology Research, 2023 The mortality rates of gastric cancer remain high due to limited therapeutic strategies. As a highly selective inhibitor of the BD2 domain of BET family proteins, ABBV-744 has potent chemotherapeutic activity against various human solid tumors.
Kun Wang +9 more
doaj +1 more source
Targeted therapy of TERT-rearranged neuroblastoma with BET bromodomain inhibitor and proteasome inhibitor combination therapy [PDF]
, 2021 Purpose: TERT gene rearrangement with transcriptional super-enhancers leads to TERT overexpression and neuroblastoma. No targeted therapy is available for clinical trials in patients with TERT-rearranged neuroblastoma.
Nelson, Christopher +37 more
core +2 more sources