Results 41 to 50 of about 14,237 (205)
Multicomponent Stapling of Glucagon‐Like Peptide‐1 Enables Receptor‐Guided PROTAC Delivery
Angewandte Chemie, EarlyView.We report a stapled glucagon‐like peptide‐1 (GLP‐1) analogue created via multicomponent tryptophan‐mediated Petasis reaction (TMPR). This strategy yields a stabilised peptide with superior helicity and improved potency. Conjugation to a bromodomain‐containing protein 4 (BRD4) degrader creates the first GLP‐1‐guided targeted protein degrader (PROTAC ...
Jan L. Venne +5 more
wiley +2 more sources
Journal of Nanobiotechnology, 2022 Although combination chemoimmunotherapy shows promising clinical results for cancer treatment, this approach is largely restricted by variable objective response rate and severe systemic adverse effects of immunotherapeutic antibody and chemotherapeutic ...
Jun Gu +9 more
doaj +1 more source
PLoS Pathogens, 2016 The human HSV-1 and -2 are common pathogens of human diseases. Both host and viral factors are involved in HSV lytic infection, although detailed mechanisms remain elusive.
Ke Ren +8 more
doaj +1 more source
VDAC1 is regulated by BRD4 and contributes to JQ1 resistance in breast cancer
Oncology Letters, 2019 Voltage-dependent anion channels (VDACs) are situated in the outer membrane of the mitochondria and serve as gatekeepers that control metabolite and ion exchange between the cytosol and mitochondria. VDAC1 is one of the most studied members of the VDAC protein family and is overexpressed in multiple types of cancer.
Yang, Guochao +7 more
openaire +3 more sources
Open Access Could Transform Drug Discovery: A Case Study of JQ1 [PDF]
Expert Opinion on Drug Discovery, 2016 The cost to develop a new drug from target discovery to market is a staggering $1.8 billion, largely due to the very high attrition rate of drug candidates and the lengthy transition times during development. Open access is an emerging model of open innovation that places no restriction on the use of information and has the potential to accelerate the ...
Arshad Z +9 more
openaire +3 more sources
JQ1 as a BRD4 Inhibitor Blocks Inflammatory Pyroptosis-Related Acute Colon Injury Induced by LPS
Frontiers in Immunology, 2021 Endotoxemia is a severe inflammation response induced by infection especially bacterial endotoxin translocation, which severely increases mortality in combination with acute colon injury.
Ling Chen +11 more
doaj +1 more source
, 2019 Programmed cell death ligand 1 (PD-L1) blockade has achieved great success in cancer immunotherapy; however, the response of triple-negative breast cancer (TNBC) to PD-L1 antibodies is limited.
Xiang Liao (628942) +7 more
core +1 more source
Effects of BRD4 inhibitor JQ1 on the expression profile of super-enhancer related lncRNAs and mRNAs in cervical cancer HeLa cells [PDF]
PeerJObjective To investigate the effects of bromine domain protein 4 (BRD4) inhibitor JQ1 on the expression profile of super-enhancer-related lncRNAs (SE-lncRNAs) and mRNAs in cervical cancer (CC) HeLa-cells. Methods The CCK8 method was implemented to detect
Jianqing Zheng +3 more
doaj +2 more sources
Targeting Hippo coactivator YAP1 through BET bromodomain inhibition in esophageal adenocarcinoma
Molecular Oncology, 2020 Hippo/YAP1 signaling is a major regulator of organ size, cancer stemness, and aggressive phenotype. Thus, targeting YAP1 may provide a novel therapeutic strategy for tumors with high YAP1 expression in esophageal cancer (EC).
Shumei Song +14 more
doaj +1 more source
Cell Death Discovery, 2023 Bromo- and extra-terminal domain (BET) inhibitors (BETi) have been shown to decrease tumor growth in preclinical models and clinical trials. However, toxicity and rapid emergence of resistance have limited their clinical implementation. To identify state
Xi Li +6 more
doaj +1 more source