Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy

Mitragynine (MG) is an indole alkaloid from kratom plant that binds opioid receptors and as such presents a scaffold for the development of atypical opioid receptor modulators. Here, the authors report a synthetic method for selective functionalization of the C11 position of MG, and show that this p...

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Autores principales: Srijita Bhowmik, Juraj Galeta, Václav Havel, Melissa Nelson, Abdelfattah Faouzi, Benjamin Bechand, Mike Ansonoff, Tomas Fiala, Amanda Hunkele, Andrew C. Kruegel, John. E. Pintar, Susruta Majumdar, Jonathan A. Javitch, Dalibor Sames
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Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/ea38af09c9b14aa088b91f729a3dae52
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spelling oai:doaj.org-article:ea38af09c9b14aa088b91f729a3dae522021-12-02T17:45:15ZSite selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy10.1038/s41467-021-23736-22041-1723https://doaj.org/article/ea38af09c9b14aa088b91f729a3dae522021-06-01T00:00:00Zhttps://doi.org/10.1038/s41467-021-23736-2https://doaj.org/toc/2041-1723Mitragynine (MG) is an indole alkaloid from kratom plant that binds opioid receptors and as such presents a scaffold for the development of atypical opioid receptor modulators. Here, the authors report a synthetic method for selective functionalization of the C11 position of MG, and show that this position is essential for fine-tuning opioid receptor signaling efficacy.Srijita BhowmikJuraj GaletaVáclav HavelMelissa NelsonAbdelfattah FaouziBenjamin BechandMike AnsonoffTomas FialaAmanda HunkeleAndrew C. KruegelJohn. E. PintarSusruta MajumdarJonathan A. JavitchDalibor SamesNature PortfolioarticleScienceQENNature Communications, Vol 12, Iss 1, Pp 1-14 (2021)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Srijita Bhowmik
Juraj Galeta
Václav Havel
Melissa Nelson
Abdelfattah Faouzi
Benjamin Bechand
Mike Ansonoff
Tomas Fiala
Amanda Hunkele
Andrew C. Kruegel
John. E. Pintar
Susruta Majumdar
Jonathan A. Javitch
Dalibor Sames
Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
description Mitragynine (MG) is an indole alkaloid from kratom plant that binds opioid receptors and as such presents a scaffold for the development of atypical opioid receptor modulators. Here, the authors report a synthetic method for selective functionalization of the C11 position of MG, and show that this position is essential for fine-tuning opioid receptor signaling efficacy.
format article
author Srijita Bhowmik
Juraj Galeta
Václav Havel
Melissa Nelson
Abdelfattah Faouzi
Benjamin Bechand
Mike Ansonoff
Tomas Fiala
Amanda Hunkele
Andrew C. Kruegel
John. E. Pintar
Susruta Majumdar
Jonathan A. Javitch
Dalibor Sames
author_facet Srijita Bhowmik
Juraj Galeta
Václav Havel
Melissa Nelson
Abdelfattah Faouzi
Benjamin Bechand
Mike Ansonoff
Tomas Fiala
Amanda Hunkele
Andrew C. Kruegel
John. E. Pintar
Susruta Majumdar
Jonathan A. Javitch
Dalibor Sames
author_sort Srijita Bhowmik
title Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
title_short Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
title_full Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
title_fullStr Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
title_full_unstemmed Site selective C–H functionalization of Mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
title_sort site selective c–h functionalization of mitragyna alkaloids reveals a molecular switch for tuning opioid receptor signaling efficacy
publisher Nature Portfolio
publishDate 2021
url https://doaj.org/article/ea38af09c9b14aa088b91f729a3dae52
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