Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia

TRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-lasting analgesia without changing mice body...

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Main Authors: Heng Zhang, Jia-Jia Lin, Ya-Kai Xie, Xiu-Zu Song, Jia-Yi Sun, Bei-Lei Zhang, Yun-Kun Qi, Zhen-Zhong Xu, Fan Yang
Format: Article
Language:English
Published: Nature Portfolio 2023-01-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-022-34817-1
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author Heng Zhang
Jia-Jia Lin
Ya-Kai Xie
Xiu-Zu Song
Jia-Yi Sun
Bei-Lei Zhang
Yun-Kun Qi
Zhen-Zhong Xu
Fan Yang
author_facet Heng Zhang
Jia-Jia Lin
Ya-Kai Xie
Xiu-Zu Song
Jia-Yi Sun
Bei-Lei Zhang
Yun-Kun Qi
Zhen-Zhong Xu
Fan Yang
author_sort Heng Zhang
collection DOAJ
description TRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-lasting analgesia without changing mice body temperature.
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spelling doaj.art-4f6d4493ac1f4d9c9aa5df9ee8c2731d2023-01-08T12:15:45ZengNature PortfolioNature Communications2041-17232023-01-0114111210.1038/s41467-022-34817-1Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesiaHeng Zhang0Jia-Jia Lin1Ya-Kai Xie2Xiu-Zu Song3Jia-Yi Sun4Bei-Lei Zhang5Yun-Kun Qi6Zhen-Zhong Xu7Fan Yang8Department of Biophysics, Kidney Disease Center of the First Affiliated Hospital, Zhejiang University School of MedicineLiangzhu Laboratory, Zhejiang University Medical CenterLiangzhu Laboratory, Zhejiang University Medical CenterDepartment of Dermatology, The Third People’s Hospital of HangzhouDepartment of Dermatology, The Third People’s Hospital of HangzhouDepartment of Dermatology, The Third People’s Hospital of HangzhouDepartment of Medicinal Chemistry, School of Pharmacy, Qingdao UniversityLiangzhu Laboratory, Zhejiang University Medical CenterDepartment of Biophysics, Kidney Disease Center of the First Affiliated Hospital, Zhejiang University School of MedicineTRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-lasting analgesia without changing mice body temperature.https://doi.org/10.1038/s41467-022-34817-1
spellingShingle Heng Zhang
Jia-Jia Lin
Ya-Kai Xie
Xiu-Zu Song
Jia-Yi Sun
Bei-Lei Zhang
Yun-Kun Qi
Zhen-Zhong Xu
Fan Yang
Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
Nature Communications
title Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
title_full Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
title_fullStr Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
title_full_unstemmed Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
title_short Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia
title_sort structure guided peptide engineering of a positive allosteric modulator targeting the outer pore of trpv1 for long lasting analgesia
url https://doi.org/10.1038/s41467-022-34817-1
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