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 …

Multisteric TRPV1 nocisensor: a target for analgesics

J Szolcsányi, Z Sándor - Trends in pharmacological sciences, 2012 - cell.com
Cloning of the transient receptor potential vanilloid type 1 (TRPV1), the heat-gated cation
channel/capsaicin receptor expressed by sensory neurons, has opened the door for …

[BOEK][B] Mammalian transient receptor potential (TRP) cation channels

B Nilius, V Flockerzi - 2014 - Springer
When we edited in 2007 the first issue on transient receptor potential channel in the
Handbook of Experimental Pharmacology, we were all very excited by the progress in this …

Capsaicin interaction with TRPV1 channels in a lipid bilayer: molecular dynamics simulation

SM Hanson, S Newstead, KJ Swartz, MSP Sansom - Biophysical journal, 2015 - cell.com
Transient receptor potential vanilloid subtype 1 (TRPV1) is a heat-sensitive ion channel also
involved in pain sensation, and is the receptor for capsaicin, the active ingredient of hot chili …

Pharmacology of the capsaicin receptor, transient receptor potential vanilloid type-1 ion channel

I Nagy, D Friston, JS Valente, JVT Perez… - Capsaicin as a …, 2014 - Springer
The capsaicin receptor, transient receptor potential vanilloid type 1 ion channel (TRPV1),
has been identified as a polymodal transducer molecule on a sub-set of primary sensory …

Functionally important amino acid residues in the transient receptor potential vanilloid 1 (TRPV1) ion channel-an overview of the current mutational data

Z Winter, A Buhala, F Ötvös, K Jósvay… - Molecular …, 2013 - journals.sagepub.com
This review aims to create an overview of the currently available results of site-directed
mutagenesis studies on transient receptor potential vanilloid type 1 (TRPV1) receptor …

Insights from molecular dynamics simulations of TRPV1 channel modulators in pain

V Dewaker, AR Sharma, U Debnath, ST Park… - Drug Discovery …, 2023 - Elsevier
TRPV1 is a nonselective cation channel vital for detecting noxious stimuli (heat, acid,
capsaicin). Its role in pain makes it a potential drug target for chronic pain management …

A new era for the design of TRPV1 antagonists and agonists with the use of structural information and molecular docking of capsaicin-like compounds

J Caballero - Journal of enzyme inhibition and medicinal chemistry, 2022 - Taylor & Francis
The design of TRPV1 antagonists and agonists has reached a new era since TRPV1
structures at near-atomic resolution are available. Today, the ligand-binding forms of several …

TRPV1: Receptor structure, activation, modulation and role in neuro-immune interactions and pain

TKE Maximiano, JA Carneiro, V Fattori, WA Verri Jr - Cell Calcium, 2024 - Elsevier
In the 1990s, the identification of a non-selective ion channel, especially responsive to
capsaicin, revolutionized the studies of somatosensation and pain that were to follow. The …

Transient receptor potential vanilloid type 1 antagonists: a patent review (2011–2014)

Y Lee, S Hong, M Cui, PK Sharma, J Lee… - Expert opinion on …, 2015 - Taylor & Francis
Introduction: Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation
channel that can be activated by noxious heat, low pH and vanilloid compounds such as …