Results 141 to 149 of about 151 (149)

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

British Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton, Fraser Nunn, Erika Lace, Álvaro Lorente‐Macías, Rachel Toth, Asier Unciti‐Broceta, Tim G. Hales   +6 more
wiley   +1 more source

Repurposed catechol‐O‐methyltransferase inhibitors tolcapone and entacapone preferentially suppress aggregation and seeding of P301 mutant tau in human neuronal models

British Journal of Pharmacology, EarlyView.
Background and purpose Pathogenic aggregation and propagation of seed‐competent TAU assemblies drive tauopathies. MAPT P301 mutations accelerate aggregation and enhance seed competence, yet pharmacological strategies selectively targeting these pathogenic species remain limited.
Ihor Kozlov, Yu‐Sheng Hung, Sudeep Roy, Alladi Charanraj Goud, Roman Kouřil, Yu‐Hui Wong, Viswanath Das   +6 more
wiley   +1 more source

Highly potent, brain‐penetrant EP2 receptor antagonists for the treatment of permanent focal cerebral ischaemia in male and female mice

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Cerebral ischaemia is a leading cause of death in older adults and imposes a substantial global economic burden. Recent studies indicate that inhibiting the Gαs‐coupled EP2 receptor reduces ischaemic brain injury by modulating neuroinflammation.
Zhen Jin, Chenyao Jiang, Eun Bee Cho, M. Dennis Leo, Jiukuan Hao, Jiawang Liu, Ying Yu, Jianxiong Jiang   +7 more
wiley   +1 more source

The Role of IGF2BP3‐Mediated Immune Response Activation in Enhancing Immunotherapy of Koumine for Gastric Cancer

Cancer Science, EarlyView.
Koumine binds IGF2BP3 and promotes its proteasomal degradation, reducing m6A on EED mRNA, accelerating EED decay, lowering H3K27me3, and promoting IRF transcription, thereby restoring MHC‐I and enhancing CD8+ T cell killing. ABSTRACT Resistance to immune checkpoint blockade in gastric cancer often arises from defective antigen presentation due to MHC‐I
Qiu Hongqiang, Lin Hailing, Lou Luqi, Wang Linyao, Lin Tian, Shengjie Zhu, Zhang Dongmei, Chen Rong, Mao Yunyi, Wancai Que, Yu Cheng   +10 more
wiley   +1 more source

Dietary Leucine Restriction Suppresses Platelet‐Driven HCC Growth by Attenuating mTOR Signaling

Cancer Science, EarlyView.
Platelets induce leucine accumulation in HCC cells. In vitro, leucine deprivation or S6K1 inhibition with PF‐4708671 suppresses platelet‐promoted proliferation, migration, and invasion. In vivo, dietary leucine restriction reduces tumor growth following platelet pre‐incubation.
Xeulian Ruan, Guiyong Ou, Cuiju Mo, Yi Zhang, Shanzi Qin, Yongling Chen, Dan Li, Liuying Nie, Li Xie, Zuojian Hu   +9 more
wiley   +1 more source

Delipidisation of wool fibres and the subsequent beneficial properties of delipidised wool fibres

Coloration Technology, EarlyView.
Abstract Wool fibres are complex matrices of proteins and fatty acids/lipids found both internally and externally. 18‐methyleicosanoic acid (18‐MEA) is covalently bound to the surface of the fibre via a thio‐ester link, and is considered one of the most important lipids as it is responsible for the hydrophobic properties of wool fibres.
Jamie A. Hawkes, David M. Lewis
wiley   +1 more source

Lactate‐Primed NETosis Modulates Hepatic Regeneration During Acute Liver Failure via the TLR9/KLF15/AJUBA Axis

Cell Proliferation, EarlyView.
This study elucidates a novel Kupffer cell‐neutrophil‐hepatocyte axis that drives metabolic‐immune crosstalk during acute liver failure. Specifically, lactate‐primed NETs release links metabolic reprogramming to NETosis‐induced regenerative failure in hepatocytes via the TLR9/KLF15/AJUBA axis.
Jin Guo, Xiaoya Zhang, Danmei Zhang, Chunxia Shi, Luwen Wang, Zuojiong Gong   +5 more
wiley   +1 more source

1H NMR metabolomics and lipidomics analysis of neutrophils reveals biomarkers of ageing, inflammageing and frailty

The FEBS Journal, EarlyView.
Using 1H NMR metabolomics, we measured polar and lipid metabolites from human blood neutrophils from people with frailty (n = 31, mean age 84Y), people with rheumatoid arthritis (n = 16, mean age 55Y), robust older (n = 24, mean age 66Y) and healthy younger people (n = 21, mean age 22Y).
Genna Ali Abdullah, Grace Filbertine, Lucy Gill, Asangaedem Akpan, Marie M. Phelan, Helen Louise Wright   +5 more
wiley   +1 more source

Iloperidone treatment mitigates the Juvenile Huntington's Disease phenotype possibly via Sigma‐1 Receptor Modulation

The FEBS Journal, EarlyView.
We investigated the potential of iloperidone as an activator of Sigma‐1 receptor (S1R) neuroprotective function in juvenile Huntington's disease (jHD). We tested iloperidone on cortical neurons differentiated from patient‐derived iPSCs, demonstrating that it acts as a S1R agonist, decreasing apoptosis, huntingtin aggregation, and oxidative stress ...
Ersilia Fornetti, Gaia Galluzzi, Mario Frezzini, Cécile Exertier, Vittorio Brufani, Gianni Colotti, Giancarlo Ruocco, Jessica Rosati, Angelo Luigi Vescovi, Daniele Narzi, Ilaria Genovese, Andrea Ilari   +11 more
wiley   +1 more source