Results 131 to 140 of about 121,181 (303)

Advances in the Structural Basis of GluN2A-Selective Negative Allosteric Modulators

ACS Medicinal Chemistry Letters
N-Methyl-d-aspartate receptors (NMDARs) are ligand-gated ion channels that play a critical role in synaptic plasticity, learning, and memory in the central nervous system (CNS). These receptors assemble into functionally diverse complexes composed of GluN1, GluN2, and GluN3 subunits.
Yinlong Li, Hongjie Yuan, Steven H. Liang   +2 more
openaire   +2 more sources

The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned fear

, 2014
The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned ...
CE Handford (15829580), Jee Hyun Kim (13075509), S Tan (13447968), AJ Lawrence (5578280)   +3 more
core  

Mechanozyme: An Artificial Enzyme With a Mechanophore Framework

Advanced Science, EarlyView.
Mechanical destabilization of a G‐quadruplex mechanophore in a DNAzyme markedly boosts its catalytic activity, demonstrating “mechanozymes” as artificial enzymes whose functions are modulated by mechanical stress exerted by ultrasonication. This mechanozyme principle is broadly applicable to control biomolecular activities.
Jiahao Ji, Pravin Pokhrel, Sajan Shakya, Bishal Pokhrel, Grinsun Sharma, Pratiksha Chaudhary, Hao Shen, Hanbin Mao   +7 more
wiley   +1 more source

Anti-stress neuropharmacological mechanisms and targets for addiction treatment: A translational framework

Neurobiology of Stress, 2018
Stress-related substance use is a major challenge for treating substance use disorders. This selective review focuses on emerging pharmacotherapies with potential for reducing stress-potentiated seeking and consumption of nicotine, alcohol, marijuana ...
Mark K. Greenwald
doaj   +1 more source

A Robust Process for an mGluR5 Negative Allosteric Modulator: Difluoromethylation and Sonogashira Coupling on Large Scale

, 2016
The development of the potent and selective mGluR5 negative allosteric modulator (NAM) 1 is described. Key features in the process, which has been implemented on a multikilogram scale, include a high-temperature difluoromethylation reaction, a ...
Mahmut Levent (2023186), Mousumi Ghosh (306838), Steven M. Hoagland (2023183), Richard J. Varsolona (1458094), Roger M. Farr (2023180), Jeffrey B. Sperry (1702318), Karen Sutherland (1458145)   +6 more
core   +1 more source

Understanding the Catalytic Determinant role of Diaphorase‐Like Subunit in Formate Dehydrogenases via Redox Couples

Advanced Science, EarlyView.
A unique mechanism of catalytic bias regulated by diaphorase‐like subunit in formate dehydrogenase from Rhodobacter aestuarii is revealed. The diaphorase‐like subunit functions act as a biological “voltage rheostat” that controls the slow release of NADH to regulate redox balance, biasing the enzyme's catalytic preference toward CO2 reduction over ...
Kuncheng Zhang, Weisong Liu, Hao Su, Huijuan Cui, Yuanming Wang, Zhiguang Zhu, Chun You, Lingling Zhang   +7 more
wiley   +1 more source

A Non‐Canonical Core Transcriptional Regulatory Circuit Orchestrates Chromatin Reprogramming to Drive Osimertinib Resistance in Non‐Small Cell Lung Cancer

Advanced Science, EarlyView.
A non‐canonical core transcriptional regulatory circuit, composed of ID3, SMAD3, and NR2F2, drives Osimertinib resistance in non‐small cell lung cancer through super‐enhancer‐mediated activation of EPAS1, which couples neuroendocrine differentiation with ferroptosis evasion.
Aochu Liu, Zhenguo Liu, Lizhen Jiang, Andong Huang, Xinqing Lin, Xinyue Li, Bingyuan Liu, Shiwen Hu, Qiang Pan, Junjun Huang, Liyuan Yin, Liling Jiang, Wei Yi, Wenjun Mao, Yueyuan Zheng, Xianping Shi   +15 more
wiley   +1 more source

Allosteric Regulation of Photophysics and Binding in Oxazine‐macrocycle Complexes at Single‐molecule Resolution

Angewandte Chemie, EarlyView.
This work explores the interactions between the oxazine dye ATTO655 and two macrocyclic hosts using optical (single‑molecule) spectroscopy. Although ATTO655 forms a classical inclusion complex with cucurbit[8]uril (CB8), its interaction with p‑sulfonatocalix[4]arene (sCX4) leads to the formation of dim exclusion complexes.
Siyu Lu, Thomas‐Otavio Peulen, Hongbin Wu, Florian Lindemann, Despoina Kapiki, Rasmus Linser, Andreas Hennig, Thorben Cordes   +7 more
wiley   +2 more sources

Novel binding mode for negative allosteric NMDA receptor modulators

Journal of General Physiology
NMDA-type ionotropic glutamate receptors mediate excitatory neurotransmission and synaptic plasticity, but aberrant signaling by these receptors is also implicated in brain disorders. Here, we present the binding site and the mechanism of action for UCM-101, a novel negative NMDA receptor modulator that produces full inhibition of NMDA receptor ...
James S. Lotti, Jed T. Syrenne, Avery J. Benton, Ahmad Al-Mousawi, Lauren E. Cornelison, Christopher J. Trolinder, Feng Yi, Zhucheng Zhang, Cindee K. Yates-Hansen, Levi J. McClelland, James Bosco, Andrew R. Rau, Rasmus P. Clausen, Kasper B. Hansen   +13 more
openaire   +2 more sources

Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage. [PDF]

, 2017
Pepcan-12 (RVD-hemopressin; RVDPVNFKLLSH) is the major peptide of a family of endogenous peptide endocannabinoids (pepcans) shown to act as negative allosteric modulators (NAM) of cannabinoid CB1 receptors.
Chicca, Andrea, Sandra Glasmacher, Glasmacher, Sandra Patricia, Zongxian Cao, Gertsch, Jürg, Pacher, Pal, Jürg Gertsch, Paloczi, Janos, Cao, Zongxian, Janos Paloczi, Vanessa Petrucci, Pal Pacher, Andrea Chicca, Petrucci, Vanessa   +13 more
core   +1 more source