Photoaffinity labeling in target-and binding-site identification

E Smith, I Collins - Future medicinal chemistry, 2015 - Taylor & Francis
Photoaffinity labeling (PAL) using a chemical probe to covalently bind its target in response
to activation by light has become a frequently used tool in drug discovery for identifying new …

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 …

Current state of potential mechanisms supporting low intensity focused ultrasound for neuromodulation

J Dell'Italia, JL Sanguinetti, MM Monti… - Frontiers in human …, 2022 - frontiersin.org
Low intensity focused ultrasound (LIFU) has been gaining traction as a non-invasive
neuromodulation technology due to its superior spatial specificity relative to transcranial …

Understanding the bases of function and modulation of α7 nicotinic receptors: implications for drug discovery

J Corradi, C Bouzat - Molecular pharmacology, 2016 - Elsevier
The nicotinic acetylcholine receptor (nAChR) belongs to a superfamily of pentameric ligand-
gated ion channels involved in many physiologic and pathologic processes. Among …

Current advances of carbene-mediated photoaffinity labeling in medicinal chemistry

SS Ge, B Chen, YY Wu, QS Long, YL Zhao, PY Wang… - RSC …, 2018 - pubs.rsc.org
Photoaffinity labeling (PAL) in combination with a chemical probe to covalently bind its target
upon UV irradiation has demonstrated considerable promise in drug discovery for identifying …

Recent advances in target characterization and identification by photoaffinity probes

J Sumranjit, SJ Chung - Molecules, 2013 - mdpi.com
Target identification of biologically active molecules such as natural products, synthetic
small molecules, peptides, and oligonucleotides mainly relies on affinity chromatography …

Allosteric modulation of nicotinic acetylcholine receptors

A Chatzidaki, NS Millar - Biochemical pharmacology, 2015 - Elsevier
Nicotinic acetylcholine receptors (nAChRs) are receptors for the neurotransmitter
acetylcholine and are members of the 'Cys-loop'family of pentameric ligand-gated ion …

Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel

L Sauguet, RJ Howard, L Malherbe, US Lee… - Nature …, 2013 - nature.com
Ethanol alters nerve signalling by interacting with proteins in the central nervous system,
particularly pentameric ligand-gated ion channels. A recent series of mutagenesis …

Specificity of Intersubunit General Anesthetic-binding Sites in the Transmembrane Domain of the Human α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor*♦

DC Chiara, SS Jayakar, X Zhou, X Zhang… - Journal of Biological …, 2013 - ASBMB
GABA type A receptors (GABA AR), the brain's major inhibitory neurotransmitter receptors,
are the targets for many general anesthetics, including volatile anesthetics, etomidate …