Sensory TRP channels in three dimensions

MM Diver, JV Lin King, D Julius… - Annual review of …, 2022 - annualreviews.org
Transient receptor potential (TRP) ion channels are sophisticated signaling machines that
detect a wide variety of environmental and physiological signals. Every cell in the body …

Transient receptor potential ankyrin 1 (TRPA1) modulators: Recent update and future perspective

Z Hu, Y Zhang, W Yu, J Li, J Yao, J Zhang… - European Journal of …, 2023 - Elsevier
The transient receptor potential ankyrin 1 (TRPA1) channel is a non-selective cation channel
that senses irritant chemicals. Its activation is closely associated with pain, inflammation, and …

Data-driven multi-objective optimization tactics for catalytic asymmetric reactions using bisphosphine ligands

JJ Dotson, L van Dijk, JC Timmerman… - Journal of the …, 2022 - ACS Publications
Optimization of the catalyst structure to simultaneously improve multiple reaction objectives
(eg, yield, enantioselectivity, and regioselectivity) remains a formidable challenge. Herein …

Redefining the synthetic logic of medicinal chemistry. Photoredox-catalyzed reactions as a general tool for aliphatic core functionalization

DF Fernández, M González-Esguevillas, S Keess… - Organic …, 2023 - ACS Publications
C (sp3)-rich aliphatic motifs in drug molecules are strongly associated with clinical success.
Historically, the availability of compound libraries based on C (sp3)-rich cores has been …

[HTML][HTML] Molecular architecture and gating mechanisms of the Drosophila TRPA1 channel

X Wang, Y Li, H Wei, Z Yang, R Luo, Y Gao, W Zhang… - Cell Discovery, 2023 - nature.com
The transient receptor potential channel subfamily A member 1 (TRPA1) ion channel is an
evolutionary conserved polymodal sensor responding to noxious temperature or chemical …

[HTML][HTML] Higenamine attenuates neuropathic pain by inhibition of NOX2/ROS/TRP/P38 mitogen-activated protein kinase/NF-ĸB signaling pathway

B Yang, S Ma, C Zhang, J Sun, D Zhang… - Frontiers in …, 2021 - frontiersin.org
Oxidative stress damage is known as one of the important factors that induce neuropathic
pain (NP). Using antioxidant therapy usually achieves an obvious curative effect and …

[HTML][HTML] Room temperature synthesis of bioactive 1, 2, 4-oxadiazoles

SV Baykov, AA Shetnev, AV Semenov… - International Journal of …, 2023 - mdpi.com
1, 2, 4-Oxadiazole is an essential motif in drug discovery represented in many experimental,
investigational, and marketed drugs. This review covers synthetic methods that allow the …

Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory …

JA Terrett, JQ Ly, P Katavolos… - Journal of Medicinal …, 2024 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium ion channel highly
expressed in the primary sensory neurons, functioning as a polymodal sensor for …

[HTML][HTML] Targeting TRP channels: recent advances in structure, ligand binding, and molecular mechanisms

J Huang, A Korsunsky, M Yazdani… - Frontiers in Molecular …, 2024 - frontiersin.org
Transient receptor potential (TRP) channels are a large and diverse family of
transmembrane ion channels that are widely expressed, have important physiological roles …

Discovery of BAY-390, a selective CNS penetrant chemical probe as transient receptor potential ankyrin 1 (TRPA1) antagonist

S Mesch, D Walter, A Laux-Biehlmann… - Journal of Medicinal …, 2023 - ACS Publications
Transient receptor potential ankyrin 1 (TRPA1) is a voltage-dependent, ligand-gated ion
channel, and activation thereof is linked to a variety of painful conditions. Preclinical studies …