Results 101 to 110 of about 37,458 (256)

Conformational Transduction Amplification in a Biomimetic Polyelectrolyte for Ultrasensitive Imaging of Iron Metabolism

Advanced Science, EarlyView.
This work designs a peptide‐free polyelectrolyte with stable, switchable conformations and near‐infrared fluorescence in water. It harnesses a cooperative Fe3+‐triggered sheet‐to‐helix transition to generate nonlinear fluorescence quenching, enabling the ultrasensitive, real‐time visualization of Fe3+ ion distribution and metabolic trafficking at ...
Yeqiang Zhou, Danqi Yang, Yiwei Wang, Shuangyan Li, Fan Fan, Jiayu Zou, Cheng Zhang, Yang Liu, Hong Tan, Mingming Ding   +9 more
wiley   +1 more source

A three-level regulatory mechanism of the aldo-keto reductase subfamily AKR12D

Nature Communications
Modulation of protein function through allosteric regulation is central in biology, but biomacromolecular systems involving multiple subunits and ligands may exhibit complex regulatory mechanisms at different levels, which remain poorly understood. Here,
Zhihong Xiao, Jinyin Zha, Xu Yang, Tingting Huang, Shuxin Huang, Qi Liu, Xiaozheng Wang, Jie Zhong, Jianting Zheng, Rubing Liang, Zixin Deng, Jian Zhang, Shuangjun Lin, Shaobo Dai   +13 more
doaj   +1 more source

Citrus aurantium honey‐mediated gut homeostasis and anti‐inflammation via Thorl/Nprl2‐TORC1 signaling: Network pharmacology and Drosophila validation

Animal Models and Experimental Medicine, EarlyView.
The study employed a four‐tiered strategy: (1) UHPLC‐FTMS profiling of Citrus aurantium honey to characterize its chemical composition; (2) network pharmacology analysis integrating target prediction, protein–protein interaction networks, and KEGG pathway enrichment to identify the Thor1/Nprl2‐TORC1 axis as a key mechanistic pathway; (3) in vitro ...
Wenqi Wan, Ruiguang Huang, Shuqiong Cao, Luxia Pan, Wenkai Zhang, Wujun Jiang, Zhiyong Liu   +6 more
wiley   +1 more source

Allosteric activation of the glutamate receptor mGlu2 by the serotonin receptor 5-HT2A

Nature Communications
G protein-coupled receptor (GPCR) dimers and higher-order oligomers are the subject of intense debates. The complexes formed between two or more different GPCRs enable the cell to integrate several signals.
Siyu Gai, Li Lin, Jiyong Meng, Yichen Wu, Li Xue, Chanjuan Xu, Qian Sun, Adrià Ricarte, James Dalton, Pedro Renault, Jesús Giraldo, Jean-Philippe Pin, Philippe Rondard, Jianfeng Liu   +13 more
doaj   +1 more source

Anxiety disorders and GABA neurotransmission: a disturbance of modulation

Neuropsychiatric Disease and Treatment, 2015
Philippe Nuss1,21Department of Psychiatry, Hôpital St Antoine, AP-HP, 2UMR 7203, INSERM ERL 1057 – Bioactive Molecules Laboratory, Pierre and Marie Curie University, Paris, FranceAbstract: Lines of evidence coming from many branches of ...
Nuss P
doaj  

Determination of the Cannabinoid CB1 Receptor’s Positive Allosteric Modulator Binding Site through Mutagenesis Studies

Pharmaceuticals
Positive allosteric modulators (PAMs) of the cannabinoid CB1 receptor (CB1) offer potential therapeutic advantages in the treatment of neuropathic pain and addiction by avoiding the adverse effects associated with orthosteric CB1 activation.
Hayley M. Green, Daniel M. J. Fellner, David B. Finlay, Daniel P. Furkert, Michelle Glass   +4 more
doaj   +1 more source

Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase

Journal of Enzyme Inhibition and Medicinal Chemistry
Cell division cycle 7 kinase (CDC7) has been found overexpressed in many cancer cell lines being also one of the kinases involved in the nuclear protein TDP-43 phosphorylation in vivo.
Elisa Rojas-Prats, Loreto Martinez-Gonzalez, Carmen Gil, David Ramírez, Ana Martinez   +4 more
doaj   +1 more source

An Agonist/Antagonist Photo‐Switchable Vitamin D Mimetic Enables Bidirectional Optical Control of VDR

Angewandte Chemie International Edition, EarlyView.
Vitamin D exhibits complex and cell‐specific biological effects in multiple tissues via activation of the ligand‐sensing transcription factor vitamin D receptor (VDR). The photo‐switchable vitamin D mimetic 10 transitions between VDR antagonist (E) and agonist (Z) activity upon illumination and offers unprecedented bidirectional optical control over ...
Xiu Ge, Sabine Willems, Francesco Melfi, Tufan Mukhopadhyay, Johannes Morstein, Jordan Artzy, Loris Knümann, Giorgia Sbriccoli, Jörg Pabel, Julian A. Marschner, Dirk Trauner, Daniel Merk   +11 more
wiley   +1 more source

Zuranolone: A case study in (regulatory) rush to judgement?

British Journal of Clinical Pharmacology, EarlyView.
Abstract Sage, in collaboration with Biogen, submitted a new drug approval for zuranolone for postpartum depression (PPD) and major depressive disorder (MDD) in December 2022. In August 2023, the US Food and Drug Administration granted approval for PPD but denied approval for MDD.
Lisa Cosgrove, Milutin Kostic, Barbara Mintzes, Gianna D'Ambrozio, Allen Shaughnessy   +4 more
wiley   +1 more source

Multi‐Scale Hybrid Modeling to Predict Cell Culture Process With Metabolic Phase Transitions

Biotechnology and Bioengineering, EarlyView.
ABSTRACT To advance understanding of cellular metabolism and reduce batch‐to‐batch variability in cell culture processes, this study introduces a multi‐scale hybrid modeling framework designed to simulate and predict the dynamic behavior of CHO cell cultures undergoing metabolic phase transitions.
Keqi Wang, Sarah W. Harcum, Wei Xie
wiley   +1 more source