期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 23, 期 20, 页码 -出版社
MDPI
DOI: 10.3390/ijms232012501
关键词
odorant receptors; ECL3; ligand selectivity; molecular modeling; functional assays
资金
- Fondation Roudnitska under the aegis of Fondation de France
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education [2020R1A6A1A03040516, 2020R1A2C2005174]
- National Research Foundation of Korea [2020R1A2C2005174] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Mammals recognize chemicals in the air via G protein-coupled odorant receptors (ORs). In addition to their orthosteric binding site, the third extracellular loop (ECL3) of these receptors contributes to ligand recognition and receptor activation.
Mammals recognize chemicals in the air via G protein-coupled odorant receptors (ORs). In addition to their orthosteric binding site, other segments of these receptors modulate ligand recognition. Focusing on human hOR1A1, which is considered prototypical of class II ORs, we used a combination of molecular modeling, site-directed mutagenesis, and in vitro functional assays. We showed that the third extracellular loop of ORs (ECL3) contributes to ligand recognition and receptor activation. Indeed, site-directed mutations in ECL3 showed differential effects on the potency and efficacy of both carvones, citronellol, and 2-nonanone.
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