Results 141 to 150 of about 306,671 (274)

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

open access: yesHepatology, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli   +13 more
wiley   +1 more source

DualPG‐DTA: A Large Language Model‐Powered Graph Neural Network Framework for Enhanced Drug‐Target Affinity Prediction and Discovery of Novel CDK9 Inhibitors Exhibiting in Vivo Anti‐Leukemia Activity

open access: yesAdvanced Science, EarlyView.
This study introduces DualPG‐DTA, a framework integrating two pre‐trained models to generate molecular and protein representations. It constructs dual graphs processed by specialized neural networks with dynamic attention for feature fusion, achieving superior benchmark performance.
Yihao Chen   +7 more
wiley   +1 more source

Emergence of highly profibrotic and proinflammatory Lrat+Fbln2+ HSC subpopulation in alcoholic hepatitis

open access: yesHepatology, EarlyView., 2022
Lrat+ quiescent hepatic stellate cells (qHSC) give rise to Lrat+Fbln2+ activated HSC (aHSC) in alcohol‐associated hepatitis and this subpopulation is highly profibrotic, inflammatory, and immunoregulatory based on their single cell transcriptomic profile. Abstract Background and Aims Relative roles of HSCs and portal fibroblasts in alcoholic hepatitis (
Steven Balog   +12 more
wiley   +1 more source

Consequences of Discontinuing a 4/6 Cyclin D-Dependent Kinase Inhibitor During Endocrine Treatment in Hormone-Sensitive Metastatic Breast Cancer Patients in the Context of the COVID-19 Outbreak. [PDF]

open access: yesClin Breast Cancer, 2023
Martin S   +10 more
europepmc   +1 more source

Dual Targeting of Tau Kinases and Autophagy by Abemaciclib Independent of CDK4/6 Inhibition

open access: yesAdvanced Science, EarlyView.
Abemaciclib rescues cognitive function and attenuates tau pathology in Alzheimer's disease models, but not through its known cancer‐fighting mechanism. This study demonstrates that abemaciclib operates independently of CDK4/6 inhibition, instead directly targeting tau kinases CaMKII and GSK3β while simultaneously promoting autophagic clearance of ...
Jihui Han   +9 more
wiley   +1 more source

TP53 R249S mutation in hepatic organoids captures the predisposing cancer risk

open access: yesHepatology, EarlyView., 2022
The systematic approach in elucidating the gain‐of‐function (GOF) roles of TP53 mutations in early liver carcinogenesis. Unique downstream targets of TP53 L3 mutations were identified from chormatin immunoprecipitation sequencing in HCC cell lines, followed by a series of validation assays to substantiate the exclusive transcriptional regulations ...
Yin Kau Lam   +10 more
wiley   +1 more source

Effectiveness of Multivitamins vs Folic Acid on Prevention of Neural Tube Defects in Mouse Genetic Models and Human Organoids

open access: yesAdvanced Science, EarlyView.
Folic acid (FA) and multivitamins/minerals (MVM) are recommended for the prevention of neural tube defects (NTDs). Using a novel human neural tube‐like organoid system and mouse models, the study compares the effectiveness of two supplements on NTDs and cellular behaviors.
Huili Li   +3 more
wiley   +1 more source

Home - About - Disclaimer - Privacy