Selective activation of TRPA1 ion channels by nitrobenzene skin sensitizers DNFB and DNCB.


Journal

The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R

Informations de publication

Date de publication:
02 2022
Historique:
received: 07 08 2021
revised: 17 12 2021
accepted: 28 12 2021
pubmed: 2 1 2022
medline: 30 4 2022
entrez: 1 1 2022
Statut: ppublish

Résumé

2, 4-dinitrofluorobenzene (DNFB) and 2, 4-dinitrochlorobenzene (DNCB) are well known as skin sensitizers that can cause dermatitis. DNFB has shown to more potently sensitize skin; however, how DNFB and DNCB cause skin inflammation at a molecular level and why this difference in their sensitization ability is observed remain unknown. In this study, we aimed to identify the molecular targets and mechanisms on which DNFB and DNCB act. We used a fluorescent calcium imaging plate reader in an initial screening assay before patch-clamp recordings for validation. Molecular docking in combination with site-directed mutagenesis was then carried out to investigate DNFB and DNCB binding sites in the TRPA1 ion channel that may be selectively activated by these tow sensitizers. We found that DNFB and DNCB selectively activated TRPA1 channel with EC

Identifiants

pubmed: 34973335
pii: S0021-9258(21)01365-X
doi: 10.1016/j.jbc.2021.101555
pmc: PMC8800105
pii:
doi:

Substances chimiques

Dinitrochlorobenzene 0
TRPA1 Cation Channel 0
TRPA1 protein, human 0
Dinitrofluorobenzene D241E059U6

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

101555

Informations de copyright

Copyright © 2021 The Authors. Published by Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Conflict of interest The authors declare that they have no conflicts of interest with the contents of this article.

Auteurs

Han Wu (H)

Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, China.

Canyang Niu (C)

Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, China.

Yaxuan Qu (Y)

Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, China.

Xiaoying Sun (X)

Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, China; Institute of Innovative Drugs, Qingdao University, Qingdao, China. Electronic address: xiaoyingsun@qdu.edu.cn.

KeWei Wang (K)

Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, China; Institute of Innovative Drugs, Qingdao University, Qingdao, China. Electronic address: wangkw@qdu.edu.cn.

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Classifications MeSH