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Medientyp:
E-Artikel
Titel:
Identification of a putative binding site critical for general anesthetic activation of TRPA1
Beteiligte:
Ton, Hoai T.;
Phan, Thieu X.;
Abramyan, Ara M.;
Shi, Lei;
Ahern, Gerard P.
Erschienen:
Proceedings of the National Academy of Sciences, 2017
Erschienen in:Proceedings of the National Academy of Sciences
Sprache:
Englisch
DOI:
10.1073/pnas.1618144114
ISSN:
0027-8424;
1091-6490
Entstehung:
Anmerkungen:
Beschreibung:
<jats:title>Significance</jats:title>
<jats:p>General anesthetics are an important class of drugs that suppress the activity of neurons in the brain to produce reversible unconsciousness. In addition, several general anesthetics, including the intravenous drug, propofol, and the inhaled gas, isoflurane, cause pain/irritation upon administration and a reduction in blood pressure. These side effects arise from activation of the transient receptor potential ankyrin repeat 1 (TRPA1) ion channel but the underlying mechanisms are unknown. In this study we identify a potential binding pocket for propofol and isoflurane, including several critical amino acid residues, located in the channel pore region of TRPA1. These results confirm an important role for the pore region in regulating channel activity. Further, the information may be useful in designing drugs to counter anesthetic-mediated activation of TRPA1.</jats:p>