Acid potentiation of the capsaicin receptor determined by a key extracellular site

SE Jordt, M Tominaga, D Julius - Proceedings of the …, 2000 - National Acad Sciences
… activity was localized to an extracellular Glu residue (E600) in the … key regulatory site of
the receptor by setting sensitivity to other noxious stimuli in response to changes in extracellular

Capsaicin receptor: TRPV1 a promiscuous TRP channel

SC Pingle, JA Matta, GP Ahern - … Receptor Potential (TRP) Channels, 2007 - Springer
… observation, several intracellular binding sites have been identified; amino acids residues
Arg-114 in the amino-terminus and Glu-761 in the carboxy-terminus play a key role in ligand …

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
… In contrast to the extracellular sites for protonation, the site … in sensing and maintaining
extracellular and intracellular pH. … Further study has localised key residues that determine …

Extracellular cations sensitize and gate capsaicin receptor TRPV1 modulating pain signaling

GP Ahern, IM Brooks, RL Miyares… - Journal of …, 2005 - Soc Neuroscience
… To confirm an action at proton-binding sites, we used mutant receptors lacking acidic
extracellular amino acids identified as a key for proton activation and modulation. E600 is believed …

Novel gating and sensitizing mechanism of capsaicin receptor (TRPV1): tonic inhibitory regulation of extracellular sodium through the external protonation sites on …

T Ohta, T Imagawa, S Ito - Journal of Biological Chemistry, 2008 - ASBMB
… ), TRPV1 is considered to be a key component of signal transduction … sites via protein
kinase C and protein kinase A downstream of activation of GTP-binding protein-coupling receptor

Understand spiciness: mechanism of TRPV1 channel activation by capsaicin

F Yang, J Zheng - Protein & cell, 2017 - Springer
… Though the capsaicin receptor is known to function as TRPV1 … to extracellular pore domain
of the channel, while capsaicin … S2 to S4 segments are key to capsaicin binding, while the …

Resiniferatoxin binds to the capsaicin receptor (TRPV1) near the extracellular side of the S4 transmembrane domain

MZ Chou, T Mtui, YD Gao, M Kohler, RE Middleton - Biochemistry, 2004 - ACS Publications
… The capsaicin binding site has been partially localized to the intracellular loop between the
… TRPV1 and the gut: from a tasty receptor for a painful vanilloid to a key player in hyperalgesia…

Capsaicin, transient receptor potential (TRP) protein subfamilies and the particular relationship between capsaicin receptors and small primary sensory neurons

H Nakagawa, A Hiura - Anatomical science international, 2006 - Wiley Online Library
… The identification of [ 3 H]-RTX binding sites on the … ages and IB4-positive neurons play a
key role in acute noxious heat … Our knowledge of intracellular signaling pathways in nociceptive …

Functional analysis of capsaicin receptor (vanilloid receptor subtype 1) multimerization and agonist responsiveness using a dominant negative mutation

EV Kuzhikandathil, H Wang, T Szabo… - Journal of …, 2001 - Soc Neuroscience
… To confirm that the vanilloid binding site is intact, we compared [ 3 H]RTX binding in wild-…
Asp) in putative extracellular domains of VR1 were mutated demonstrated that a key glutamine …

Capsaicin Receptor TRPV1: Biophysics, Physiology, and Pharmacology

S Li, J Zheng - Capsaicinoids: From Natural Sources to Biosynthesis …, 2024 - Springer
… observations that capsaicin can activate TRPV1 from both intracellular and extracellular sides…
modeling and mutagenesis tests, it was proposed that capsaicin takes a “head-down tail-up…