Transient receptor potential channels as drug targets: from the science of basic research to the art of medicine

B Nilius, A Szallasi, DR Sibley - Pharmacological reviews, 2014 - Elsevier
The large Trp gene family encodes transient receptor potential (TRP) proteins that form
novel cation-selective ion channels. In mammals, 28 Trp channel genes have been …

Phosphoinositides: tiny lipids with giant impact on cell regulation

T Balla - Physiological reviews, 2013 - journals.physiology.org
Phosphoinositides (PIs) make up only a small fraction of cellular phospholipids, yet they
control almost all aspects of a cell's life and death. These lipids gained tremendous research …

Structural basis of the activation of TRPV5 channels by long-chain acyl-Coenzyme-A

BH Lee, JJ De Jesús Pérez, V Moiseenkova-Bell… - Nature …, 2023 - nature.com
Long-chain acyl-coenzyme A (LC-CoA) is a crucial metabolic intermediate that plays
important cellular regulatory roles, including activation and inhibition of ion channels. The …

Opening of the human epithelial calcium channel TRPV6

LL McGoldrick, AK Singh, K Saotome… - Nature, 2018 - nature.com
Calcium-selective transient receptor potential vanilloid subfamily member 6 (TRPV6)
channels play a critical role in calcium uptake in epithelial tissues,,,. Altered TRPV6 …

Molecular pathway and structural mechanism of human oncochannel TRPV6 inhibition by the phytocannabinoid tetrahydrocannabivarin

A Neuberger, YA Trofimov, MV Yelshanskaya… - Nature …, 2023 - nature.com
The calcium-selective oncochannel TRPV6 is an important driver of cell proliferation in
human cancers. Despite increasing interest of pharmacological research in developing …

Structural insights on TRPV5 gating by endogenous modulators

TET Hughes, RA Pumroy, AT Yazici… - Nature …, 2018 - nature.com
TRPV5 is a transient receptor potential channel involved in calcium reabsorption. Here we
investigate the interaction of two endogenous modulators with TRPV5. Both …

PIP2 depletion promotes TRPV4 channel activity in mouse brain capillary endothelial cells

OF Harraz, TA Longden, D Hill-Eubanks, MT Nelson - Elife, 2018 - elifesciences.org
We recently reported that the inward-rectifier Kir2. 1 channel in brain capillary endothelial
cells (cECs) plays a major role in neurovascular coupling (NVC) by mediating a neuronal …

Structural mechanisms of TRPV6 inhibition by ruthenium red and econazole

A Neuberger, KD Nadezhdin, AI Sobolevsky - Nature Communications, 2021 - nature.com
TRPV6 is a calcium-selective ion channel implicated in epithelial Ca2+ uptake. TRPV6
inhibitors are needed for the treatment of a broad range of diseases associated with …

Structural mechanism of human oncochannel TRPV6 inhibition by the natural phytoestrogen genistein

A Neuberger, YA Trofimov, MV Yelshanskaya… - Nature …, 2023 - nature.com
Calcium-selective oncochannel TRPV6 is the major driver of cell proliferation in human
cancers. While significant effort has been invested in the development of synthetic TRPV6 …

Phosphoinositide regulation of TRP channels: A functional overview in the structural era

T Rohacs - Annual Review of Physiology, 2024 - annualreviews.org
Transient receptor potential (TRP) ion channels have diverse activation mechanisms
including physical stimuli, such as high or low temperatures, and a variety of intracellular …