Multitargeting nature of muscarinic orthosteric agonists and antagonists
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj +1 more source
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements [PDF]
Label-free biosensor technology based on dynamic mass redistribution (DMR) of cellular constituents promises to translate GPCR signaling into complex optical 'fingerprints' in real time in living cells.
Blattermann, S+16 more
core +1 more source
Sympathetic nerve innervation promotes the progression of Epstein‐Barr virus‐positive diffuse large B‐cell lymphoma (EBV+ DLBCL) via β2‐adrenergic receptors. The discovery of enhanced nerve infiltration and β2AR expression reveals a novel mechanism and highlights the sympathetic–β2AR axis as a promising target for therapeutic intervention in EBV+ DLBCL.
Silan Huang+10 more
wiley +1 more source
Genetics‐Based Targeting Strategies for Precise Neuromodulation
In this Review, the fundamental principles and implementation protocols of genetics‐based precision neuromodulation are first introduced. Then, wireless and low‐invasive strategies based on nano‐transducing materials are highlighted, along with a dissection and analysis of the strengths and weaknesses of representative studies.
Yuyuan He+11 more
wiley +1 more source
Pro-inflammatory mechanisms of muscarinic receptor stimulation in airway smooth muscle
Background Acetylcholine, the primary parasympathetic neurotransmitter in the airways, plays an important role in bronchoconstriction and mucus production.
Zuyderduyn Suzanne+8 more
doaj +1 more source
Inhibition of Subsets of G Protein-coupled Receptors by Empty Mutants of G Protein α Subunits in Go, G11, and G16 [PDF]
We previously reported that the xanthine nucleotide binding Goα mutant, GoαX, inhibited the activation of Gi-coupled receptors. We constructed similar mutations in G11α and G16α and characterized their nucleotide binding and receptor interaction.
Gu, Lingjie, Simon, Melvin I., Yu, Bo
core +1 more source
New Horizons for Multiple Sclerosis Therapy: 2025 and Beyond
The advances achieved against multiple sclerosis (MS) represent one of the great success stories of modern molecular medicine. The development of therapies with increasing selectivity and safety, guided by gains in understanding the fundamental immunology, neurobiology, genetics, and triggers of this disease, have broadened the traditional focus on ...
Joseph J. Sabatino Jr.+2 more
wiley +1 more source
Acetylcholine and the activation of muscarinic receptors influence the activity of neural networks generating locomotor behaviour in the mammalian spinal cord.
Sandrine S Bertrand+1 more
doaj +1 more source
HL-1 cells express an inwardly rectifying K+ current activated via muscarinic receptors comparable to that in mouse atrial myocytes [PDF]
An inwardly rectifying K^+ current is present in atrial cardiac myocytes that is activated by acetylcholine (I_{KACh}). Physiologically, activation of the current in the SA node is important in slowing the heart rate with increased parasympathetic tone ...
A Benians+44 more
core +2 more sources
A Cholinergic Synaptically Triggered Event Participates in the Generation of Persistent Activity Necessary for Eye Fixation [PDF]
An exciting topic regarding integrative properties of the nervous system is how transient motor commands or brief sensory stimuli are able to evoke persistent neuronal changes, mainly as a sustained, tonic action potential firing.
Alvarado, Juan Carlos+5 more
core +3 more sources