Results 161 to 170 of about 121,181 (303)

A neurotensin receptor type 1-derived pepducin acts as a biased allosteric modulator to regulate target receptor function

Acta Pharmaceutica Sinica B
Pepducins are synthetic membrane-tethered lipopeptides designed to allosterically modulate G protein-coupled receptor (GPCR) signaling. Here, we characterize a series of pepducins targeting the neurotensin receptor type 1 (NTSR1), revealing their complex
Rebecca L. Brouillette, Frédérique Lussier, Émile Breault, Nathan Meneboo, Malihe Hassanzadeh, Victoria Tremblay, Magali Chartier, Élora Midavaine, Laurence Ulrich, Jérôme Côté, Véronique Blais, Christine E. Mona, Jean-Michel Longpré, Michel Grandbois, Pierre-Luc Boudreault, Martin Audet, Élie Besserer-Offroy, Philippe Sarret   +17 more
doaj   +1 more source

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

Novel RXFP3 negative allosteric modulator RLX-33 reduces alcohol self-administration in rats. [PDF]

J Neurochem, 2023
Van Voorhies KJ, Liu W, Lovelock DF, Lin S, Liu J, Guan D, Gay EA, Jin C, Besheer J.   +8 more
europepmc   +1 more source

The First Negative Allosteric Modulator for Dopamine D 2 and D 3 Receptors SB269652 May Lead to a New Generation of Antipsychotic Drugs MOL #107607 2 RUNNING TITLE PAGE Running title: Allosteric modulators as new generation antipsychotics

, 2020
Until recently, the only strategy to develop drugs regulating GPCR activity was through the identification of compounds that directly acted on the orthosteric sites for endogenous ligands.
Irene Fasciani, Mario Rossi, Francesco Marampon, Marco Scarselli, Roberto Maggio   +4 more
core  

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

Development of a Dihydroquinoline-Pyrazoline GluN2C/2D-Selective Negative Allosteric Modulator of the N-Methyl-d-aspartate Receptor. [PDF]

ACS Chem Neurosci, 2023
D'Erasmo MP, Akins NS, Ma P, Jing Y, Swanger SA, Sharma SK, Bartsch PW, Menaldino DS, Arcoria PJ, Bui TT, Pons-Bennaceur A, Le P, Allen JP, Ullman EZ, Nocilla KA, Zhang J, Perszyk RE, Kim S, Acker TM, Taz A, Burton SL, Coe K, Fritzemeier RG, Burnashev N, Yuan H, Liotta DC, Traynelis SF.   +26 more
europepmc   +1 more source

Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype [PDF]

ACS Medicinal Chemistry Letters, 2013
openaire   +2 more sources

Molecular Modeling Study of a Receptor–Orthosteric Ligand–Allosteric Modulator Signaling Complex

Allosteric modulators (AMs) are considered as a perpetual hotspot in research for their higher selectivity and various effects on orthosteric ligands (OL).
Yixuan Hao (13933634), Xiang-Qun Xie (1319565), Yuanqiang Wang (3184182), Chih-Jung Chen (207116), Zhiwei Feng (117939), Yasmin Othman (13933637), Chen Jiang (200126), Jiayi Yuan (5520836), Xibing He (1351038)   +8 more
core   +1 more source

Harnessing ferroptosis from multilayer defense networks to nanoplatforms for specific cancer therapy

BMEMat, EarlyView.
Nanomaterials target metabolically‐regulated ferroptosis for cancer therapy. Iron‐based or alternative nanoplatforms integrate ferroptosis with chemotherapy, immunotherapy, or radiotherapy. They enable stimulus‐responsive therapies (photothermal, photodynamic, sonodynamic) activated by near‐infrared, light, or ultrasound, achieving potent synergistic ...
Xinyue Xu, Xuejian Wang, Wenyan Jiang, Wan Hairul Anuar Kamaruddin, Chunyan Fang, Pengfei Zhang   +5 more
wiley   +1 more source