Medicinal chemistry, pharmacology, and clinical implications of TRPV1 receptor antagonists

M Aghazadeh Tabrizi, PG Baraldi… - Medicinal research …, 2017 - Wiley Online Library
Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed on sensory
neurons triggering an influx of cations. TRPV1 receptors function as homotetramers …

Involvement of P2X7 receptors in chronic pain disorders

WJ Ren, P Illes - Purinergic Signalling, 2022 - Springer
Chronic pain is caused by cellular damage with an obligatory inflammatory component. In
response to noxious stimuli, high levels of ATP leave according to their concentration …

Structural snapshots of TRPV1 reveal mechanism of polymodal functionality

K Zhang, D Julius, Y Cheng - Cell, 2021 - cell.com
Many transient receptor potential (TRP) channels respond to diverse stimuli and
conditionally conduct small and large cations. Such functional plasticity is presumably …

Glia accumulate evidence that actions are futile and suppress unsuccessful behavior

Y Mu, DV Bennett, M Rubinov, S Narayan, CT Yang… - Cell, 2019 - cell.com
When a behavior repeatedly fails to achieve its goal, animals often give up and become
passive, which can be strategic for preserving energy or regrouping between attempts. It is …

Structure of the full-length TRPV2 channel by cryo-EM

KW Huynh, MR Cohen, J Jiang, A Samanta… - Nature …, 2016 - nature.com
Transient receptor potential (TRP) proteins form a superfamily Ca2+-permeable cation
channels regulated by a range of chemical and physical stimuli. Structural analysis of a …

Structural insights into the gating mechanisms of TRPV channels

RA Pumroy, EC Fluck III, T Ahmed… - Cell Calcium, 2020 - Elsevier
Abstract Transient Receptor Potential channels from the vanilloid subfamily (TRPV) are a
group of cation channels modulated by a variety of endogenous stimuli as well as a range of …

Physical basis of apparent pore dilation of ATP-activated P2X receptor channels

M Li, GES Toombes, SD Silberberg, KJ Swartz - Nature neuroscience, 2015 - nature.com
The selectivity of ion channels is fundamental for their roles in electrical and chemical
signaling and in ion homeostasis. Although most ion channels exhibit stable ion selectivity …

Conformational plasticity in the selectivity filter of the TRPV2 ion channel

L Zubcevic, S Le, H Yang, SY Lee - Nature Structural & Molecular …, 2018 - nature.com
Transient receptor potential vanilloid (TRPV) channels are activated by ligands and heat
and are involved in various physiological processes. In contrast to the architecturally related …

[HTML][HTML] TRP channels in calcium homeostasis: from hormonal control to structure-function relationship of TRPV5 and TRPV6

MKC van Goor, JGJ Hoenderop… - Biochimica et Biophysica …, 2017 - Elsevier
Maintaining plasma calcium levels within a narrow range is of vital importance for many
physiological functions. Therefore, calcium transport processes in the intestine, bone and …

Sequence and structural conservation reveal fingerprint residues in TRP channels

D Cabezas-Bratesco, FA Mcgee, CK Colenso, K Zavala… - Elife, 2022 - elifesciences.org
Transient receptor potential (TRP) proteins are a large family of cation-selective channels,
surpassed in variety only by voltage-gated potassium channels. Detailed molecular …