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 …

Optical control of neuronal ion channels and receptors

P Paoletti, GCR Ellis-Davies, A Mourot - Nature Reviews Neuroscience, 2019 - nature.com
Light-controllable tools provide powerful means to manipulate and interrogate brain function
with relatively low invasiveness and high spatiotemporal precision. Although optogenetic …

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 …

Harnessing allostery: a novel approach to drug discovery

S Lu, S Li, J Zhang - Medicinal research reviews, 2014 - Wiley Online Library
Allostery is the most direct and efficient way for regulation of biological macromolecule
function, ranging from the control of metabolic mechanisms to signal transduction pathways …

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 …

Optical Control of Invertebrate nAChR and Behaviors with Dithienylethene-Imidacloprid

Q Xu, C Zhang, Z Xu, L Wang, Z Liu, Z Li… - Journal of Agricultural …, 2023 - ACS Publications
Photopharmacology involving azobenzene or dithienylethene has changed established
methods of studying receptor functions, allowing for increasing the spatiotemporal …

Crystallographic studies of pharmacological sites in pentameric ligand-gated ion channels

L Sauguet, A Shahsavar, M Delarue - Biochimica et Biophysica Acta (BBA) …, 2015 - Elsevier
Background Pentameric ligand-gated ion channels (pLGICs) mediate fast chemical
transmission of nerve signals in the central and peripheral nervous system. On the functional …

Identification of the binding site of chroman-4-one-based sirtuin 2-selective inhibitors using photoaffinity labeling in combination with tandem mass spectrometry

T Seifert, M Malo, J Lengqvist, C Sihlbom… - Journal of Medicinal …, 2016 - ACS Publications
Photoaffinity labeling (PAL) was used to identify the binding site of chroman-4-one-based
SIRT2-selective inhibitors. The photoactive diazirine 4, a potent SIRT2 inhibitor, was …

Advances in the In vitro and In vivo pharmacology of Alpha4beta2 nicotinic receptor positive allosteric modulators

JL Wilkerson, F Deba, ML Crowley, AK Hamouda… - …, 2020 - Elsevier
Receptors containing α4 and β2 subunits are a major neuronal nicotinic acetylcholine
receptor (nAChR) subtype in the brain. This receptor plays a critical role in nicotine …

Multiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy

P Iturriaga-Vásquez, J Alzate-Morales… - Pharmacological …, 2015 - Elsevier
For decades, the development of selective compounds has been the main goal for chemists
and biologists involved in drug discovery. However, diverse lines of evidence indicate that …