International Union of Basic and Clinical Pharmacology. CX. Classification of receptors for 5-hydroxytryptamine; pharmacology and function

NM Barnes, GP Ahern, C Becamel, J Bockaert… - Pharmacological …, 2021 - Elsevier
HT receptors expressed throughout the human body are targets for established therapeutics
and various drugs in development. Their diversity of structure and function reflects the …

Therapeutic potential of pyrrole and pyrrolidine analogs: an update

N Jeelan Basha, SM Basavarajaiah, K Shyamsunder - Molecular Diversity, 2022 - Springer
The chemistry of nitrogen-containing heterocyclic compound pyrrole and pyrrolidine has
been a versatile field of study for a long time for its diverse biological and medicinal …

Structure and gating mechanism of the α7 nicotinic acetylcholine receptor

CM Noviello, A Gharpure, N Mukhtasimova, R Cabuco… - Cell, 2021 - cell.com
The α7 nicotinic acetylcholine receptor plays critical roles in the central nervous system and
in the cholinergic inflammatory pathway. This ligand-gated ion channel assembles as a …

Structural mechanism of muscle nicotinic receptor desensitization and block by curare

MM Rahman, T Basta, J Teng, M Lee… - Nature structural & …, 2022 - nature.com
Binding of the neurotransmitter acetylcholine to its receptors on muscle fibers depolarizes
the membrane and thereby triggers muscle contraction. We sought to understand at the level …

The nicotinic acetylcholine receptor and its pentameric homologs: toward an allosteric mechanism of signal transduction at the atomic level

M Cecchini, PJ Corringer… - Annual Review of …, 2024 - annualreviews.org
The nicotinic acetylcholine receptor has served, since its biochemical identification in the
1970s, as a model of an allosteric ligand-gated ion channel mediating signal transition at the …

Agonist selectivity and ion permeation in the α3β4 ganglionic nicotinic receptor

A Gharpure, J Teng, Y Zhuang, CM Noviello, RM Walsh… - Neuron, 2019 - cell.com
Nicotinic acetylcholine receptors are pentameric ion channels that mediate fast chemical
neurotransmission. The α3β4 nicotinic receptor subtype forms the principal relay between …

Direct structural insights into GABAA receptor pharmacology

JJ Kim, RE Hibbs - Trends in biochemical sciences, 2021 - cell.com
GABA A receptors are pentameric ligand-gated ion channels that mediate most fast
neuronal inhibition in the brain. In addition to their important physiological roles, they are …

Conformational transitions and ligand-binding to a muscle-type nicotinic acetylcholine receptor

E Zarkadas, E Pebay-Peyroula, MJ Thompson… - Neuron, 2022 - cell.com
Fast synaptic communication requires receptors that respond to the presence of
neurotransmitter by opening an ion channel across the post-synaptic membrane. The …

Megabodies expand the nanobody toolkit for protein structure determination by single-particle cryo-EM

T Uchański, S Masiulis, B Fischer, V Kalichuk… - Nature …, 2021 - nature.com
Nanobodies are popular and versatile tools for structural biology. They have a compact
single immunoglobulin domain organization, bind target proteins with high affinities while …

Mechanism of gating and partial agonist action in the glycine receptor

J Yu, H Zhu, R Lape, T Greiner, J Du, W Lü, L Sivilotti… - Cell, 2021 - cell.com
Ligand-gated ion channels mediate signal transduction at chemical synapses and transition
between resting, open, and desensitized states in response to neurotransmitter binding …