Results 91 to 100 of about 139,314 (301)

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

eLife, 2017
Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type
Joan Font, Marc López-Cano, Serena Notartomaso, Pamela Scarselli, Paola Di Pietro, Roger Bresolí-Obach, Giuseppe Battaglia, Fanny Malhaire, Xavier Rovira, Juanlo Catena, Jesús Giraldo, Jean-Philippe Pin, Víctor Fernández-Dueñas, Cyril Goudet, Santi Nonell, Ferdinando Nicoletti, Amadeu Llebaria, Francisco Ciruela   +17 more
doaj   +1 more source

A negative allosteric modulator of PDE4D enhances learning after traumatic brain injury

, 2018
•A PDE4D negative allosteric modulator did not alter cognition in non-injured rats.•Cognition after TBI is improved with a PDE4D negative allosteric modulator.•A PDE4D negative allosteric modulator improves LTP in TBI animals. Traumatic brain injury (TBI)
W. Dalton Dietrich, Dale A. Calixte, Gurney, Mark E, Dietrich, W. Dalton, Atkins, Coleen M, Coleen M. Atkins, Titus, David J, Wilson, Nicole M, David J. Titus, Oscar Alcazar, Alcazar, Oscar, Nicole M. Wilson, Calixte, Dale A, Mark E. Gurney   +13 more
core   +1 more source

Effects of Ivermectin as an Allosteric Modulator of nAChRs on Dopamine Release [PDF]

, 2022
Dopamine (DA) terminals are regulated by acetylcholine activity on nicotinic receptors (nAChRs). Nicotine reduces DA release from low frequency stimulation, but enhances release at higher frequencies.
Robinson, J. Kayden, Bishop, Samantha, Foote, Sarah E., Graul, Benjamin E., Steimle, Emma, Hafen, Caylor, Yorgason, Jordan, Wadsworth, Hillary, Barlow, Joshua   +8 more
core  

Microfluidic Nano‐Assembly of Red‐Blood‐Cell (RBC) Lipids and Components for Engineering Extracellular Vesicles

Advanced Healthcare Materials, EarlyView.
Engineered red blood cell‐derived extracellular vesicles (eRBCEVs) are synthesized via controlled microfluidic assembly from native RBC lipids, enabling tunable encapsulation of proteins, nucleic acids, nanoparticles, and viral vectors. The platform demonstrates reproducible nanoscale architecture, preserved membrane composition, and functional cargo ...
Chiranth K. Nagaraj, Xilal Y. Rima, Kim T. Nguyen, Courtney Culkins, Nana Boateng, Jacob Doon‐Ralls, Alejandro Bresolin, Xin Huang, Hong Li, Vahedi Amid, Ajeet Pal Singh, Dharti Shantaram, Anastasiia Amari, Mangesh D. Hade, Nicholas R. Merriam, Zachary D. Schultz, Scott Q. Harper, Nizar Y. Saad, Setty M. Magaña, Willa A. Hsueh, Rachel E. Kopec, Blaise R. Kimmel, Andre F. Palmer, Eduardo Reátegui   +23 more
wiley   +1 more source

Vesicular glutamate release from central axons contributes to myelin damage

Nature Communications, 2018
Neuronal activity can lead to vesicular release of glutamate. Here the authors demonstrate that vesicular release of glutamate occurs in axons during ischemic conditions, and that an allosteric modulator of GluN2C/D is protective in models of ischemic ...
Sean Doyle, Daniel Bloch Hansen, Jasmine Vella, Peter Bond, Glenn Harper, Christian Zammit, Mario Valentino, Robert Fern   +7 more
doaj   +1 more source

TOLLIP Inhibits Psoriasis Progression via Suppressing PKM2‐Mediated Glycolysis in Keratinocytes

Advanced Science, EarlyView.
In this study, we identify TOLLIP as a critical regulator of psoriasis pathogenesis through its modulation of glycolytic metabolism. Our findings establish the TOLLIP‐PKM2‐glycolysis axis as a key mechanism linking metabolic reprogramming to psoriasis pathogenesis, and propose TOLLIP as a promising therapeutic target.
Xiuhuan Jiang, Guoying Miao, Na Shen, Qingxia Han, Xiaoru Han, Zichang Qiao, Kexin Feng, Zhuo Tan, Yaguang Wang, Xiuhua Liu, Chen Wu, Zhenzhen Yan   +11 more
wiley   +1 more source

Progress in GABAA receptor agonists for insomnia disorder

Frontiers in Pharmacology
Insomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health.
Weiyi Wang, Wanting Fu, Hongyan Zhu, Jing Ma, Jian Zhang, Jia Qi   +5 more
doaj   +1 more source

Concentration dependence of the interaction of two allosteric modulators binding each to its own allosteric site.

, 2019
Upper row, simulation of tracer binding (ordinate) in the presence two allosteric modulators A and B each binding to its own site, where A is either positive (left) or negative (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

Design and Engineering of an Artificial Bifunctional N‐Deacetylase/N‐Sulfotransferase for the Biosynthesis of N‐Sulfated Heparosan

Advanced Science, EarlyView.
An artificial bifunctional N‐deacetylase/N‐sulfotransferase was engineered in Escherichia coli by combining screened N‐deacetylases with an NST domain. The integrated engineering strategy improved enzyme performance. The optimized enzyme efficiently converted heparosan into N‐sulfated heparosan, addressing a key bottleneck in microbial heparin ...
Xintong Xi, Ruirui Xu, Daoan Wang, Guobin Yin, Xinjing Wang, Haiqin Chen, Guocheng Du, Jian Chen, Zhen Kang   +8 more
wiley   +1 more source

Identification of a unique Ca2+-binding site in rat acid-sensing ion channel 3

Nature Communications, 2018
Acid-sensing ion channels (ASICs) sense changes in extracellular acidity with Ca2+ as an allosteric modulator and channel blocker. Here authors use electrophysiology and molecular dynamics simulation to identify the residue in ASIC3 which modulates ...
Zhicheng Zuo, Rachel N. Smith, Zhenglan Chen, Amruta S. Agharkar, Heather D. Snell, Renqi Huang, Jin Liu, Eric B. Gonzales   +7 more
doaj   +1 more source