Towards a comprehensive understanding of anesthetic mechanisms of action: a decade of discovery

HC Hemmings, PM Riegelhaupt, MB Kelz, K Solt… - Trends in …, 2019 - cell.com
Significant progress has been made in the 21st century towards a comprehensive
understanding of the mechanisms of action of general anesthetics, coincident with progress …

Emerging molecular mechanisms of signal transduction in pentameric ligand-gated ion channels

Á Nemecz, MS Prevost, A Menny, PJ Corringer - Neuron, 2016 - cell.com
Nicotinic acetylcholine, serotonin type 3, γ-amminobutyric acid type A, and glycine receptors
are major players of human neuronal communication. They belong to the family of …

Allosteric modulation of GABAA receptors via multiple drug-binding sites

W Sieghart - Advances in pharmacology, 2015 - Elsevier
GABA A receptors are ligand-gated ion channels composed of five subunits that can be
opened by GABA and be modulated by multiple pharmacologically and clinically important …

International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric …

A Christopoulos, JP Changeux, WA Catterall… - Pharmacological …, 2014 - Elsevier
Allosteric interactions play vital roles in metabolic processes and signal transduction and,
more recently, have become the focus of numerous pharmacological studies because of the …

Multiple functional neurosteroid binding sites on GABAA receptors

ZW Chen, JR Bracamontes, MM Budelier… - PLoS …, 2019 - journals.plos.org
Neurosteroids are endogenous modulators of neuronal excitability and nervous system
development and are being developed as anesthetic agents and treatments for psychiatric …

Photoaffinity labeling chemistries used to map biomolecular interactions

AV West, CM Woo - Israel Journal of Chemistry, 2023 - Wiley Online Library
Photoaffinity labeling (PAL) is one of the few biochemical techniques that can give direct
evidence of biomolecular interactions in cells. Several photoactivatable functional groups …

Multiple Propofol-binding Sites in a γ-Aminobutyric Acid Type A Receptor (GABAAR) Identified Using a Photoreactive Propofol Analog*♦

SS Jayakar, X Zhou, DC Chiara, Z Dostalova… - Journal of Biological …, 2014 - ASBMB
Propofol acts as a positive allosteric modulator of γ-aminobutyric acid type A receptors
(GABA A Rs), an interaction necessary for its anesthetic potency in vivo as a general …

Photoaffinity labelling with small molecules

RA Homan, JD Lapek, CM Woo, S Niessen… - Nature Reviews …, 2024 - nature.com
Small molecules can serve as leads for new therapeutics as well as powerful tools to
investigate biological processes. Understanding the interactions of these molecules …

A propofol binding site in the voltage sensor domain mediates inhibition of HCN1 channel activity

V Burtscher, L Wang, J Cowgill, ZW Chen, C Edge… - Science …, 2025 - science.org
Hyperpolarization-activated and cyclic nucleotide–gated (HCN) ion channels are members
of the cyclic nucleotide–binding family and are crucial for regulating cellular automaticity in …

[HTML][HTML] Recent progress on the molecular pharmacology of propofol

P Tang, R Eckenhoff - F1000Research, 2018 - ncbi.nlm.nih.gov
The precise mechanism by which propofol enhances GABAergic transmission remains
unclear, but much progress has been made regarding the underlying structural and dynamic …