Pharmacology of TRPC channels and its potential in cardiovascular and metabolic medicine

RS Bon, DJ Wright, DJ Beech… - Annual review of …, 2022 - annualreviews.org
Transient receptor potential canonical (TRPC) proteins assemble to form homo-or
heterotetrameric, nonselective cation channels permeable to K+, Na+, and Ca2+. TRPC …

Role of Store-Operated Ca2+ Entry in the Pulmonary Vascular Remodeling Occurring in Pulmonary Arterial Hypertension

B Masson, D Montani, M Humbert, V Capuano… - Biomolecules, 2021 - mdpi.com
Pulmonary arterial hypertension (PAH) is a severe and multifactorial disease. PAH
pathogenesis mostly involves pulmonary arterial endothelial and pulmonary arterial smooth …

TRPC5 controls the adrenaline-mediated counter regulation of hypoglycemia

J Bröker-Lai, J Rego Terol, C Richter, I Mathar… - The EMBO …, 2024 - embopress.org
Hypoglycemia triggers autonomic and endocrine counter-regulatory responses to restore
glucose homeostasis, a response that is impaired in patients with diabetes and its long-term …

[HTML][HTML] DogCatcher allows loop-friendly protein-protein ligation

AH Keeble, VK Yadav, MP Ferla, CC Bauer… - Cell chemical …, 2022 - cell.com
There are many efficient ways to connect proteins at termini. However, connecting at a loop
is difficult because of lower flexibility and variable environment. Here, we have developed …

Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site

DJ Wright, KJ Simmons, RM Johnson… - Communications …, 2020 - nature.com
Abstract TRPC1/4/5 channels are non-specific cation channels implicated in a wide variety
of diseases, and TRPC1/4/5 inhibitors have recently entered clinical trials. However …

Nonselective TRPC channel inhibition and suppression of aminoglycoside-induced premature termination codon readthrough by the small molecule AC1903

A Baradaran-Heravi, CC Bauer, IB Pickles… - Journal of Biological …, 2022 - ASBMB
Nonsense mutations, which occur in∼ 11% of patients with genetic disorders, introduce
premature termination codons (PTCs) that lead to truncated proteins and promote nonsense …

BTDAzo: A photoswitchable Trpc5 channel activator

M Müller, K Niemeyer, N Urban, NK Ojha… - Angewandte …, 2022 - Wiley Online Library
Photoswitchable reagents can be powerful tools for high‐precision biological control.
TRPC5 is a Ca2+‐permeable cation channel with distinct tissue‐specific roles, from synaptic …

Schwarzinicine A inhibits transient receptor potential canonical channels and exhibits overt vasorelaxation effects

YY Mak, BJ Loong, P Millns, CC Bauer… - Phytotherapy …, 2022 - Wiley Online Library
This study investigated the vasorelaxant effects of schwarzinicine A, an alkaloid recently
reported from Ficus schwarzii Koord. Regulation of calcium homeostasis in vascular smooth …

Ideal efficacy photoswitches for TRPC4/5 channels harness high potency for spatiotemporally-resolved control of TRPC function in live tissues

M Müller, K Niemeyer, NK Ojha, SA Porav… - bioRxiv, 2024 - biorxiv.org
Directly probing the endogenous biological roles of target proteins with high spatial and
temporal resolution, as non-invasively and reproducibly as possible, is a shared conceptual …

Cryo-EM structures of human TRPC5 reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site

DJ Wright, KJ Simmons, RM Johnson, DJ Beech… - bioRxiv, 2020 - biorxiv.org
Abstract TRPC1/4/5 channels are non-specific cation channels implicated in a wide variety
of diseases, and TRPC1/4/5 inhibitors have recently entered the first clinical trials. However …