Results 51 to 60 of about 128,101 (191)

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain

, 2018
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomainsBRD2, BRD3, BRD4, and BRDTeach contain two bromodomain modules.
Chun-wa Chung (1343454), David J. Hirst (1399282), Paul Bamborough (1343466), Emmanuel H. Demont (1399288), Matthew Lindon (1355946), Robert P. Law (2613493), Rab K. Prinjha (449759), Allan J. B. Watson (1369614), Stephen J. Atkinson (1297362), Laurie J. Gordon (1343442)   +9 more
core   +2 more sources

Flavonoids as Putative Epi-Modulators: Insight into Their Binding Mode with BRD4 Bromodomains Using Molecular Docking and Dynamics

Biomolecules, 2018
Flavonoids are widely recognized as natural polydrugs, given their anti-inflammatory, antioxidant, sedative, and antineoplastic activities. Recently, different studies showed that flavonoids have the potential to inhibit bromodomain and extraterminal ...
Fernando D. Prieto-Martínez, José L. Medina-Franco   +1 more
doaj   +1 more source

Epigenetic heterogeneity and plasticity in therapy‐induced tumor states through single‐cell multi‐omics

Molecular Oncology, EarlyView.
Single‐cell multi‐omics reveals epigenetic heterogeneity across therapy‐adaptive tumor states, including quiescent/dormant, drug‐tolerant persister, and EMT‐like phenotypes. By linking regulatory features with state‐associated biomarkers, these approaches inform biomarker‐guided therapeutic strategies for evolving tumors.
Hee Jung Kim, Hwiyeong Lee, Jin Hong, Daechan Park   +3 more
wiley   +1 more source

Dietary Compound Resveratrol Is a Pan-BET Bromodomain Inhibitor [PDF]

Nutrients, 2017
The chemopreventive and anticancer effects of resveratrol (RSV) are widely reported in the literature. Specifically, mechanisms involving epigenetic regulation are promising targets to regulate tumor development. Bromodomains act as epigenetic readers by recognizing lysine acetylation on histone tails and boosting gene expression in order to regulate ...
Luiz Dutra, David Heidenreich, Gabriel Silva, Chung Man Chin, Stefan Knapp, Jean Santos   +5 more
openaire   +4 more sources

Targeting transcription factors associated with hemoglobinopathies: Lessons from successful interventions and implications for cancer

Molecular Oncology, EarlyView.
This review summarizes the transcription factors, repressive chromatin‐modifying complexes, and epigenetic mechanisms that control fetal hemoglobin repression. Notably, many regulators of γ‐globin silencing also function in transcriptional and epigenetic networks that drive cancer, highlighting opportunities to translate advances in hemoglobinopathy ...
Meigen Yu, Puspa Das, Xing Zhang, Xiaodong Cheng   +3 more
wiley   +1 more source

BET Inhibitor JQ1 Attenuates Feline Leukemia Virus DNA, Provirus, and Antigen Production in Domestic Cat Cell Lines

Viruses, 2023
Feline leukemia virus (FeLV) is a cosmopolitan gammaretrovirus that causes lifelong infections and fatal diseases, including leukemias, lymphomas, immunodeficiencies, and anemias, in domestic and wild felids.
Garrick M. Moll, Cheryl L. Swenson, Vilma Yuzbasiyan-Gurkan   +2 more
doaj   +1 more source

Histone H3K18 Lactylation Promotes the Malignant Progression of Wilms Tumor via a PSRC1/AKT/HIF‐1α Positive Feedback Loop

Advanced Science, EarlyView.
In nephroblastoma, aberrant glycolysis drives lactate accumulation, which elevates histone H3K18 lactylation via p300. Lactylation of the PSRC1 promoter activates its transcription. PSRC1 competitively binds AKT, relieving PTEN‐mediated inhibition and triggering AKT/mTOR/HIF‐1α signaling.
Yanping Wang, Hongjie Gao, Bifei Zhang, Xuetian Li, Ding Li, Aihua Cao, Fengyin Sun   +6 more
wiley   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

Advanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu, Xue Yuan, Yan Zhou, Rui Yuan, Shaocheng Xie, Yong Chen, Peiyi Wang, Jianmei Gao, Qihai Gong   +8 more
wiley   +1 more source

Targeting BET bromodomain proteins in solid tumors

Oncotarget, 2016
There is increasing interest in inhibitors targeting BET (bromodomain and extra-terminal) proteins because of the association between this family of proteins and cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression
Sahai, Vaibhav, Collier, Katharine A., Eckerdt, Frank D., Munshi, Hidayatullah G., Redig, Amanda J   +4 more
openaire   +5 more sources

Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains [PDF]

Molecular Cell, 2019
Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the interaction landscape, with three distinct ...
Lambert JP, Picaud S, Fujisawa T, Hou H, Savitsky P, Uusküla-Reimand L, Gupta GD, Abdouni H, Lin ZY, Tucholska M, Knight JDR, Gonzalez-Badillo B, St-Denis N, Newman JA, Stucki M, Pelletier L, Bandeira N, Wilson MD, Filippakopoulos P, Gingras AC   +19 more
openaire   +4 more sources