Positive and negative modulation of nicotinic receptors

HR Arias - Advances in protein chemistry and structural biology, 2010 - Elsevier
Nicotinic acetylcholine receptors (AChRs) are one of the best characterized ion channels
from the Cys-loop receptor superfamily. The study of acetylcholine binding proteins and …

Molecular mechanisms and binding site locations for noncompetitive antagonists of nicotinic acetylcholine receptors

HR Arias, P Bhumireddy, C Bouzat - … journal of biochemistry & cell biology, 2006 - Elsevier
Nicotinic acetylcholine receptors are pentameric proteins that belong to the Cys-loop
receptor superfamily. Their essential mechanism of functioning is to couple neurotransmitter …

Gating of nicotinic ACh receptors: latest insights into ligand binding and function

JL Yakel - The Journal of Physiology, 2010 - Wiley Online Library
Nicotinic acetylcholine receptors (nAChRs) are in the superfamily of cys‐loop receptors, and
are widely expressed in the nervous system where they participate in a variety of …

Designing selective modulators for the nicotinic receptor subtypes: challenges and opportunities

D Manetti, C Bellucci, N Chiaramonte… - Future Medicinal …, 2018 - Taylor & Francis
Nicotinic receptors are membrane proteins involved in several physiological processes.
They are considered suitable drug targets for various CNS disorders or conditions, as shown …

Topology of ligand binding sites on the nicotinic acetylcholine receptor

HR Arias - Brain Research Reviews, 1997 - Elsevier
The nicotinic acetylcholine receptor (AChR) presents two very well differentiated domains for
ligand binding that account for different cholinergic properties. In the hydrophilic …

Toward a structural basis for the function of nicotinic acetylcholine receptors and their cousins

A Karlin, MH Akabas - Neuron, 1995 - Elsevier
The nicotinic acetylcholine (ACh) receptors and the other neurotransmitter-gated ion
channels have key roles in fast synaptic transmission throughout the nervous system. These …

Recent advances in the discovery of nicotinic acetylcholine receptor allosteric modulators

D Manetti, S Dei, HR Arias, L Braconi, A Gabellini… - Molecules, 2023 - mdpi.com
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent
agonists, allosteric activating PAMs and neutral or silent allosteric modulators are …

Activation of the nicotinic acetylcholine receptor involves a switch in conformation of the α subunits

N Unwin, A Miyazawa, J Li, Y Fujiyoshi - Journal of molecular biology, 2002 - Elsevier
The nicotinic acetylcholine (ACh) receptor belongs to a superfamily of synaptic ion channels
that open in response to the binding of chemical transmitters. Their mechanism of activation …

Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling

RL Papke, JM Lindstrom - Neuropharmacology, 2020 - Elsevier
Postsynaptic nAChRs in the peripheral nervous system are critical for neuromuscular and
autonomic neurotransmission. Pre-and peri-synaptic nAChRs in the brain modulate …

The acetylcholine receptor ligand-gated channel as a molecular target of disease and therapeutic agents

FJ Barrantes - Neurochemical research, 1997 - Springer
Over the last two decades a convergence of techniques from various scientific disciplines
has led to enormous growth in our comprehension of the structure, evolutionary trends and …