[HTML][HTML] Advances in TRP channel drug discovery: from target validation to clinical studies

AP Koivisto, MG Belvisi, R Gaudet… - Nature reviews Drug …, 2022 - nature.com
Transient receptor potential (TRP) channels are multifunctional signalling molecules with
many roles in sensory perception and cellular physiology. Therefore, it is not surprising that …

Molecular targets of the phytocannabinoids: a complex picture

P Morales, DP Hurst, PH Reggio - Phytocannabinoids: Unraveling the …, 2017 - Springer
For centuries, hashish and marihuana, both derived from the Indian hemp Cannabis sativa
L., have been used for their medicinal, as well as, their psychotropic effects. These effects …

Heat-dependent opening of TRPV1 in the presence of capsaicin

DH Kwon, F Zhang, Y Suo, J Bouvette… - Nature structural & …, 2021 - nature.com
Transient receptor potential vanilloid member 1 (TRPV1) is a Ca2+-permeable cation
channel that serves as the primary heat and capsaicin sensor in humans. Using cryo-EM, we …

TRPV1 structures in nanodiscs reveal mechanisms of ligand and lipid action

Y Gao, E Cao, D Julius, Y Cheng - Nature, 2016 - nature.com
When integral membrane proteins are visualized in detergents or other artificial systems, an
important layer of information is lost regarding lipid interactions and their effects on protein …

Feeling nature's PAINS: natural products, natural product drugs, and pan assay interference compounds (PAINS)

JB Baell - Journal of natural products, 2016 - ACS Publications
We have previously reported on classes of compounds that can interfere with bioassays via
a number of different mechanisms and termed such compounds Pan Assay INterference …

[HTML][HTML] Chemical activation of the mechanotransduction channel Piezo1

R Syeda, J Xu, AE Dubin, B Coste, J Mathur, T Huynh… - elife, 2015 - elifesciences.org
Piezo ion channels are activated by various types of mechanical stimuli and function as
biological pressure sensors in both vertebrates and invertebrates. To date, mechanical …

TRPV1 structures in distinct conformations reveal activation mechanisms

E Cao, M Liao, Y Cheng, D Julius - Nature, 2013 - nature.com
Transient receptor potential (TRP) channels are polymodal signal detectors that respond to
a wide range of physical and chemical stimuli. Elucidating how these channels integrate and …

A nutrient-specific gut hormone arbitrates between courtship and feeding

HH Lin, MC Kuang, I Hossain, Y Xuan, L Beebe… - Nature, 2022 - nature.com
Animals must set behavioural priority in a context-dependent manner and switch from one
behaviour to another at the appropriate moment,–. Here we probe the molecular and …

Defining and assessing animal pain

LU Sneddon, RW Elwood, SA Adamo, MC Leach - Animal behaviour, 2014 - Elsevier
Highlights•Assessing pain in animals is problematic without a distinct definition.•We provide
clear criteria for animal pain that can be used to evaluate if pain occurs.•The empirical …

TRPV1-targeted drugs in development for human pain conditions

M Iftinca, M Defaye, C Altier - Drugs, 2021 - Springer
The transient receptor potential vanilloid-1 (TRPV1) is a non-specific cation channel known
for its sensitivity to pungent vanilloid compound (ie capsaicin) and noxious stimuli, including …