The Third Extracellular Loop of Mammalian Odorant Receptors Is Involved in Ligand Binding

Tammy Shim; Jody Pacalon; Won-Cheol Kim; Xiaojing Cong; Jérémie Topin; Jérôme Golebiowski; Cheil Moon

doi:10.3390/ijms232012501

Back

The Third Extracellular Loop of Mammalian Odorant Receptors Is Involved in Ligand Binding

Journal article

Open access

Peer reviewed

The Third Extracellular Loop of Mammalian Odorant Receptors Is Involved in Ligand Binding

Tammy Shim, Jody Pacalon, Won-Cheol Kim, Xiaojing Cong, Jérémie Topin, Jérôme Golebiowski and Cheil Moon

International Journal of Molecular Sciences, Vol.23(20)

2022

DOI: https://doi.org/10.3390/ijms232012501

PMCID: PMC9604345

PMID: 36293357

Abstract

odorant receptors

ECL3

ligand selectivity

molecular modeling

functional assays

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.

Files and links (2)

url

Find in HALView

url

https://doi.org/10.3390/ijms232012501View

Published (Version of record) Open

Metrics

1 Record Views

See more details

Details

Title: The Third Extracellular Loop of Mammalian Odorant Receptors Is Involved in Ligand Binding
Creators - without role: Tammy Shim - Daegu Gyeongbuk Institute of Science and Technology
Jody Pacalon - Institut de Chimie de Nice
Won-Cheol Kim - Daegu Gyeongbuk Institute of Science and Technology
Xiaojing Cong - Université de Montpellier, Institut de Génomique Fonctionnelle - IGF
Jérémie Topin - Université Côte d'Azur
Jérôme Golebiowski - Daegu Gyeongbuk Institute of Science and Technology
Cheil Moon - Daegu Gyeongbuk Institute of Science and Technology
Publication Details: International Journal of Molecular Sciences, Vol.23(20)
Grant note: In this work, J.P was supported by the Fondation Roudnitska under the aegis of Fondation de France and C.M was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (2020R1A6A1A03040516 and 2020R1A2C2005174)
Identifiers: 9940793209311
Academic Unit: Institut de Génomique Fonctionnelle - IGF
Language: English
Resource Type: Journal article
Local Fields: hal-04712540