Breaking barriers to novel analgesic drug development

AS Yekkirala, DP Roberson, BP Bean… - Nature reviews Drug …, 2017 - nature.com
Acute and chronic pain complaints, although common, are generally poorly served by
existing therapies. This unmet clinical need reflects a failure to develop novel classes of …

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 …

[HTML][HTML] Basic pharmacology of local anaesthetics

A Taylor, G McLeod - BJA education, 2020 - Elsevier
Local anaesthetic agents suppress action potentials in excitable tissues by blocking voltage-
gated Na+ channels. In doing so, they inhibit action potentials in nociceptive fibres and so …

Trpa1

PM Zygmunt, ED Högestätt - … potential (TRP) cation channels: volume I, 2014 - Springer
The transient receptor potential ankyrin subtype 1 protein (TRPA1) is a nonselective cation
channel permeable to Ca 2+, Na+, and K+. TRPA1 is a promiscuous chemical nocisensor …

The science of local anesthesia: basic research, clinical application, and future directions

P Lirk, MW Hollmann, G Strichartz - Anesthesia & Analgesia, 2018 - journals.lww.com
Local anesthetics have been used clinically for more than a century, but new insights into
their mechanisms of action and their interaction with biological systems continue to surprise …

A pain-inducing centipede toxin targets the heat activation machinery of nociceptor TRPV1

S Yang, F Yang, N Wei, J Hong, B Li, L Luo… - Nature …, 2015 - nature.com
The capsaicin receptor TRPV1 ion channel is a polymodal nociceptor that responds to heat
with exquisite sensitivity through an unknown mechanism. Here we report the identification …

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 …

Sense and immunity: context-dependent neuro-immune interplay

SL Foster, CR Seehus, CJ Woolf, S Talbot - Frontiers in immunology, 2017 - frontiersin.org
The sensory nervous and immune systems, historically considered autonomous, actually
work in concert to promote host defense and tissue homeostasis. These systems interact …

Transient receptor potential vanilloid 1 (TRPV1)‐independent actions of capsaicin on cellular excitability and ion transport

M Oz, DE Lorke, FC Howarth - Medicinal Research Reviews, 2023 - Wiley Online Library
Capsaicin is a naturally occurring alkaloid derived from chili pepper that is responsible for its
hot pungent taste. Capsaicin is known to exert multiple pharmacological actions, including …

Identification of novel high-affinity substrates of OCT1 using machine learning-guided virtual screening and experimental validation

O Jensen, J Brockmöller… - Journal of medicinal …, 2021 - ACS Publications
OCT1 is the most highly expressed cation transporter in the liver and affects
pharmacokinetics and pharmacodynamics. Newly marketed drugs have previously been …