[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 …
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 …
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
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 …
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
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 …
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 …
a number of different mechanisms and termed such compounds Pan Assay INterference …
[HTML][HTML] Chemical activation of the mechanotransduction channel Piezo1
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 …
biological pressure sensors in both vertebrates and invertebrates. To date, mechanical …
TRPV1 structures in distinct conformations reveal activation mechanisms
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 wide range of physical and chemical stimuli. Elucidating how these channels integrate and …
A nutrient-specific gut hormone arbitrates between courtship and feeding
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 …
behaviour to another at the appropriate moment,–. Here we probe the molecular and …
Defining and assessing animal pain
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 …
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
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 …
for its sensitivity to pungent vanilloid compound (ie capsaicin) and noxious stimuli, including …