Results 121 to 130 of about 121,181 (303)

Novel 1-(1-Arylimiazolin-2-Yl)-3-Arylalkilurea Derivatives with Modulatory Activity on Opioid MOP Receptors

Molecules
μ-opioid receptor ligands such as morphine and fentanyl are the most known and potent painkillers. However, the severe side effects seen with their use significantly limit their widespread use.
Dominik Straszak, Sylwia Woźniak, Agata Siwek, Monika Głuch-Lutwin, Marcin Kołaczkowski, Aldona Pietrzak, Bartłomiej Drop, Dariusz Matosiuk   +7 more
doaj   +1 more source

A novel negative allosteric modulator selective for GluN2C/2D-containing NMDA receptors inhibits synaptic transmission in hippocampal interneurons

ACS Chemical Neuroscience, 2017
N-methyl-D-aspartate receptors (NMDARs) are ionotropic glutamate receptors that mediate excitatory synaptic transmission and have been implicated in numerous neurological disorders. NMDARs typically comprise two GluN1 and two GluN2 subunits.
Sharon A. Swanger, Katie M Vance, Timothy M. Acker, S. Zimmerman, John O. DiRaddo, S. J. Myers, C. Bundgaard, Cara A Mosley, Samantha L. Summer, D. Menaldino, H. Jensen, D. Liotta, S. Traynelis   +12 more
semanticscholar   +1 more source

Dose‐Dependent Reprogramming of Chromatin Accessibility by SOX4 Drives the Transcriptional Response to Iron Overload

Advanced Science, EarlyView.
This study demonstrates that iron overload triggers widespread chromatin compaction and transcriptional repression in human granulosa cells, recapitulating features of endometriosis. The epigenetic reprogramming is orchestrated by a TFEB‐SOX4‐SWI/SNF axis, with SOX4 acting as a central, dosage‐sensitive regulator.
Feifei Li, Yaoqiu Wu, Guangyu Yang, Jingyi Lai, Xiaoyue Sun, Liyan Wang, Xiaoli Li, Jing Zhang, Qingxue Zhang, Hui Chen, Haiyan Lin, Bingxiang Xu, Junfeng Zhang, Hailong Wang, Anming Meng, Chunwei Cao   +15 more
wiley   +1 more source

The Ascaris suum nicotinic receptor, ACR-16, as a drug target: Four novel negative allosteric modulators from virtual screening

International Journal for Parasitology: Drugs and Drug Resistance, 2016
Soil-transmitted helminth infections in humans and livestock cause significant debility, reduced productivity and economic losses globally. There are a limited number of effective anthelmintic drugs available for treating helminths infections, and their ...
Fudan Zheng, Alan P. Robertson, Melanie Abongwa, Edward W. Yu, Richard J. Martin   +4 more
doaj   +1 more source

Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors.

, 2015
The mediodorsal thalamus (MD) likely plays an important role in cognition as it receives abundant afferent connections from the amygdala and prefrontal cortex (PFC).
Salt, T.E., Copeland, C.S., Neale, S.A., Neale, SA, Salt, TE, Copeland, CS   +5 more
core   +1 more source

Targeting Supramolecular Active Complexes of Nav1.7/Nav1.8 to Relieve Chronic Neuropathic Pain

Advanced Science, EarlyView.
In mice and patients with severe chronic neuropathic pain (NP), Nav1.7, Nav1.8, TrkB, and five cytoskeletal proteins form supramolecular active complexes (SMACs) with polygonal lattice structures as noxious signal amplifiers in dorsal root ganglion (DRG) neurons.
Liting Sun, Hang Xian, Yunxin Shi, Taotan Yang, Hongyan Shuai, Wenchao Hu, Siying Fei, Miao Xu, Taoyuan Yang, Ruilong Xia, Ting Wen, Fengting Zhu, Yan Fu, Yang Li, Wei Xia, Ran Qian, Yuanying Liu, Zhicheng Tian, Lamei Li, Qian Zhou, Lize Xiong, Rui Cong, Ceng Luo, Shengxi Wu, Xiafeng Shen, Xin Yu, Rou‐Gang Xie, Changgeng Peng   +27 more
wiley   +1 more source

Concentration dependence of the interaction of two allosteric modulators that compete for the same allosteric site.

, 2019
Upper row, simulation of tracer binding (ordinate) in the presence of two allosteric modulators A and B competing for the same allosteric site, where α is either less than one (left) or greater than one (right) and B is negative allosteric modulator ...
Esam E. El-Fakahany (339452), Alena Randáková (339451), Jan Jakubík (339449), Vladimír Doležal (339453)   +3 more
core   +1 more source

Divergent Roles of mGlu2 and mGlu3 Receptors in Amyloid‐β Production and Cognitive Dysfunctions in Alzheimer's Disease

Advanced Science, EarlyView.
This study explores the opposing effects of the mGluR2 and mGluR3 receptors on amyloid precursor protein processing. mGluR2 promotes amyloidogenic cleavage, while mGluR3 favors non‐amyloidogenic pathways. Using a brain‐penetrant nanobody as a mGluR2 positive allosteric modulator, the study uncovers how its chronic activation aggravates amyloid‐β burden
Pierre‐André Lafon, Mireille Elodie Tsitokana, Ugo Guy Alenda, Yen‐Ling Lian, Clémentine Eva Philibert, Mathieu Oosterlaken, Marta Cimadevila, Gaëlle Dudon, Jessica Monnic, Salomé Roux, Julie Bessié, Séverine Diem, Franck Vandermoere, Laurent Prézeau, Patrick Chames, Julie Kniazeff, Sylvie Claeysen, Anaïs Menny, Jean‐Philippe Pin, Véronique Perrier, Jianfeng Liu, Philippe Rondard   +21 more
wiley   +1 more source

Development of novel, cns penetrant mglu3 selective negative allosteric modulator probes derived from a closely related mglu5 positive allosteric modulator

, 2012
Metabotropic glutamate (mGlu) receptors are examples of family C G-protein-coupled receptors that possess vast roles in the pathophysiology of central nervous system (CNS) disorders.
Bruner, Joshua Andrew
core  

SDS‐CRISPR for Single‐Nucleotide Variant Detection

Advanced Science, EarlyView.
Structure‐disruption‐sensitive CRISPR (SDS‐CRISPR) converts structural instability into single‐nucleotide precision, thereby overcoming mismatch tolerance in canonical Cas12a and enabling versatile diagnostics across DNA, RNA, and microRNA targets. When applied to rapid IDH1 mutation detection for glioma genotyping and integrated with lateral‐flow ...
Xin Guan, Chong Guo, Jiongyu Zhang, Rui Yang, Yerramsetti Ramachandra, Chengyu Hou, Minjie Pei, Shuo Zhang, Kurt T. Schalper, Xingye Liu, Qian Wu, Ketan R. Bulsara, Changchun Liu   +12 more
wiley   +1 more source