Results 151 to 160 of about 107,657 (326)

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

Molecular Modeling Study of Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex

, 2022
Allosteric modulators (AMs) are always the hotspot in research for their higher selectivity and various effects on the orthosteric ligands (OL), whereas AMs are also classified in terms of its functionalities as positive, negative, or silent allosteric ...
Jiang, Chen
core  

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

Transformation of Pro-Leu-Gly-NH₂ Peptidomimetic Positive Allosteric Modulators of the Dopamine D₂ Receptor into Negative Modulators

, 2016
The synthesis of dimethyl derivatives of 5.6.5 spiro bicyclic lactam Pro-Leu-Gly-NH2 peptidomimetics was carried out to test the hypothesis that by placing methyl groups on the β-methylene carbon of the thiazolidine ring steric bulk would be introduced ...
Rodney L. Johnson (442506), Ram K. Mishra (442507), Swapna Bhagwanth (2091793), Satyendra Mishra (308953), Ritesh Daya (2091799), Jordan Mah (2091796)   +5 more
core   +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

The mesenchymal stem cell differentiation to osteoblasts is potentiate by the allosteric modulation of A2B adenosine receptors. [PDF]

, 2015
The A2B adenosine receptor (A2BAR) has been recently emerged as the major adenosine receptor involved in the mesenchymal stem cell differentiation to osteoblast and bone formation, highlighting this receptor as a new target in bone diseases.
GIACOMELLI, CHIARA, MARTINI, CLAUDIA, DANIELE, SIMONA, Greco, G, Cosimelli, B, Novellino, E, TALIANI, SABRINA, TRINCAVELLI, MARIA LETIZIA, NATALI, LETIZIA, DA SETTIMO PASSETTI, FEDERICO   +9 more
core  

Sustained pharmacodynamic effects of S‐ketamine on cortical excitability and resting‐state brain activity: A randomized, placebo‐controlled trial

British Journal of Clinical Pharmacology, EarlyView.
Aims This study aimed to investigate a set of pharmacodynamic biomarkers reflecting acute, delayed and sustained central nervous system effects of S‐ketamine, used as a tool compound for rapid‐acting antidepressant activity, with the goal of informing biomarker strategies for delayed antidepressant effects.
Catherine M. K. E. de Cuba, Annika A. de Goede, Joost. C. van Mechelen, Laura G. J. M. Borghans, Liam van der Aa, Erik Olofsen, Maria J. Juachon, Robert J. Doll, Amy Gillespie, Catherine J. Harmer, Gabriël E. Jacobs, Jules A. A. C. Heuberger   +11 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

Engineering Murine Cross‐Reactivity Into an Affibody to Human Death Receptor 5

Biotechnology and Bioengineering, EarlyView.
ABSTRACT Interspecies cross‐reactive protein therapeutics that target conserved epitopes across species are critical for translational research. The present study showcases the engineering of an affibody molecule, originally discovered for binding to human death receptor 5 (hDR5) with 94 nM affinity, to simultaneously acquire cross‐reactivity to murine
Tse‐Han Kuo, Nagamani Vunnam, Jonathan N. Sachs, Benjamin J. Hackel   +3 more
wiley   +1 more source