Ligand binding at the protein–lipid interface: strategic considerations for drug design

J Payandeh, M Volgraf - Nature Reviews Drug Discovery, 2021 - nature.com
Many drug targets are embedded within the phospholipid bilayer of cellular membranes,
including G protein-coupled receptors, ion channels, transporters and membrane-bound …

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 …

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 insights into opposing actions of neurosteroids on GABAA receptors

DH Legesse, C Fan, J Teng, Y Zhuang… - Nature …, 2023 - nature.com
Abstract γ-Aminobutyric acid type A (GABAA) receptors mediate fast inhibitory signaling in
the brain and are targets of numerous drugs and endogenous neurosteroids. A subset of …

Cryo-EM structures reveal native GABAA receptor assemblies and pharmacology

C Sun, H Zhu, S Clark, E Gouaux - Nature, 2023 - nature.com
Type A γ-aminobutyric acid receptors (GABAARs) are the principal inhibitory receptors in the
brain and the target of a wide range of clinical agents, including anaesthetics, sedatives …

Structural and dynamic mechanisms of GABAA receptor modulators with opposing activities

S Zhu, A Sridhar, J Teng, RJ Howard, E Lindahl… - Nature …, 2022 - nature.com
Abstract γ-Aminobutyric acid type A (GABAA) receptors are pentameric ligand-gated ion
channels abundant in the central nervous system and are prolific drug targets for treating …

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 …

Convergent resistance to GABA receptor neurotoxins through plant–insect coevolution

L Guo, X Qiao, D Haji, T Zhou, Z Liu… - Nature Ecology & …, 2023 - nature.com
The molecular mechanisms of coevolution between plants and insects remain elusive.
GABA receptors are targets of many neurotoxic terpenoids, which represent the most diverse …

A comprehensive review on pyrimidine analogs-versatile scaffold with medicinal and biological potential

J Basha, NM Goudgaon - Journal of Molecular Structure, 2021 - Elsevier
Pyrimidines are nitrogen-containing heterocycles known for anticancer, anti-HIV, antifungal,
and antibacterial activities. Pyrimidines, compounds bearing this heterocycle, are common …

[HTML][HTML] Structural mechanisms of GABAA receptor autoimmune encephalitis

CM Noviello, J Kreye, J Teng, H Prüss, RE Hibbs - Cell, 2022 - cell.com
Autoantibodies targeting neuronal membrane proteins can cause encephalitis, seizures,
and severe behavioral abnormalities. While antibodies for several neuronal targets have …