TRPV1: Structure, Endogenous Agonists, and Mechanisms.

Int J Mol Sci

Departamento de Neurociencia Cognitiva, División Neurociencias, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico.

Published: May 2020

The Transient Receptor Potential Vanilloid 1 (TRPV1) channel is a polymodal protein with functions widely linked to the generation of pain. Several agonists of exogenous and endogenous nature have been described for this ion channel. Nonetheless, detailed mechanisms and description of binding sites have been resolved only for a few endogenous agonists. This review focuses on summarizing discoveries made in this particular field of study and highlighting the fact that studying the molecular details of activation of the channel by different agonists can shed light on biophysical traits that had not been previously demonstrated.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7279265PMC
http://dx.doi.org/10.3390/ijms21103421DOI Listing

Publication Analysis

Top Keywords

endogenous agonists
8
trpv1 structure
4
structure endogenous
4
agonists
4
agonists mechanisms
4
mechanisms transient
4
transient receptor
4
receptor potential
4
potential vanilloid
4
vanilloid trpv1
4

Similar Publications

Advances in the therapeutic potentials of ligands of the apelin receptor APJ.

Eur J Pharmacol

January 2025

Department of Molecular Genetics, Groningen Biomolecular Sciences and Biotechnology Institute, University of Groningen, 9747 AG Groningen, the Netherlands. Electronic address:

Angiotensin II protein J receptor, APJ, is a type A G protein coupled receptor. Endogenous apelin and elabela peptides stimulate APJ via distinct signalling profiles. A complex signalling map of elabela-stimulated APJ was published in 2022.

View Article and Find Full Text PDF

BDNF plays a crucial role in shaping the structure and function of neurons. BDNF signaling in the dorsolateral striatum (DLS) is part of an endogenous pathway that protects against the development of alcohol use disorder (AUD). Dysregulation of BDNF levels in the cortex or dysfunction of BDNF/TrkB signaling in the DLS results in the escalation of alcohol drinking and compulsive alcohol use.

View Article and Find Full Text PDF

Circadian rhythm disorders in the blind.

Handb Clin Neurol

January 2025

Neurology Department, Adsalutem Institute Sleep Medicine, Barcelona, Spain; Neurology Service, Sleep Disorders Unit, Hospital Universitari Sagrat Cor, Grupo Quirónsalud, Barcelona, Spain.

Non-24-h sleep-wake disorder in blind patients without light perception is an orphan circadian rhythm sleep-wake disorder and is extremely rare in sighted people. Non-24-h sleep-wake disorder is characterized by insomnia and daytime sleepiness alternating with asymptomatic episodes. The frequency of symptomatic periods depends on the daily desynchronization of endogenous circadian pattern of each patient.

View Article and Find Full Text PDF

N-glycosylation of ephrin B1 modulates its function and confers therapeutic potential in B-cell lymphoma.

J Biol Chem

January 2025

State Key Laboratory of Pharmaceutical Biotechnology, Department of Biochemistry, School of Life Sciences, Nanjing University, Nanjing, 210023, China. Electronic address:

Given the pivotal role of the Eph-Ephrin signaling pathway in tumor progression, agonists or antagonists targeting Eph/Ephrin have emerged as promising anticancer strategies. However, the implications of glycosylation modifications within Eph/Ephrin and their targeted protein therapeutics remain elusive. Here, we identify that N-glycosylation within the receptor-binding domain (RBD) of ephrin B1 (EFNB1) is indispensable for its functional repertoire.

View Article and Find Full Text PDF

Cytosolic DNA composition is determined by genomic instability mechanism and regulates dendritic cell-mediated anti-tumor immunity.

Cell Rep

January 2025

Department of Oncology, Cross Cancer Institute, University of Alberta, Edmonton, AB T6G 1Z2, Canada; Department of Medical Microbiology and Immunology, University of Alberta, Edmonton, AB T6G 2R3, Canada. Electronic address:

Patients with colorectal cancers (CRCs) that have microsatellite instability (MSI) (MSI CRCs) face a better prognosis than those with the more common chromosomal instability (CIN) subtype (CIN CRCs) due to improved T cell-mediated anti-tumor immune responses. Previous investigations identified the cytosolic DNA (cyDNA) sensor STING as necessary for chemokine-mediated T cell recruitment in MSI CRCs. Here, we find that cyDNA from MSI CRC cells is inherently more capable of inducing STING activation and improves cytotoxic T cell activation by dendritic cells (DCs).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!