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A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra

Cnidarians are characterized by the possession of stinging organelles, called nematocysts, which they use for prey capture and defense. Nematocyst discharge is controlled by a mechanosensory apparatus with analogies to vertebrate hair cells. Members of the transient receptor potential (TRPN) ion cha...

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Hauptverfasser: Hofmann, Diana (VerfasserIn) , Garg, Niharika (VerfasserIn) , Grässle, Simone (VerfasserIn) , Vanderheiden, Sylvia (VerfasserIn) , Bergheim, Bruno Gideon (VerfasserIn) , Bräse, Stefan (VerfasserIn) , Jung, Nicole (VerfasserIn) , Özbek, Suat (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 18 October 2021
In: Scientific reports
Year: 2021, Jahrgang: 11, Pages: 1-11
ISSN:2045-2322
DOI:10.1038/s41598-021-99974-7
Online-Zugang:Verlag, kostenfrei, Volltext: https://doi.org/10.1038/s41598-021-99974-7
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Verfasserangaben:Diana Hofmann, Niharika Garg, Simone Grässle, Sylvia Vanderheiden, Bruno Gideon Bergheim, Stefan Bräse, Nicole Jung & Suat Özbek
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Zusammenfassung:Cnidarians are characterized by the possession of stinging organelles, called nematocysts, which they use for prey capture and defense. Nematocyst discharge is controlled by a mechanosensory apparatus with analogies to vertebrate hair cells. Members of the transient receptor potential (TRPN) ion channel family are supposed to be involved in the transduction of the mechanical stimulus. A small molecule screen was performed to identify compounds that affect nematocyst discharge in Hydra. We identified several [2.2]paracyclophanes that cause inhibition of nematocyst discharge in the low micro-molar range. Further structure-activity analyses within the compound class of [2.2] paracyclophanes showed common features that are required for the inhibitory activity of the [2.2] paracyclophane core motif. This study demonstrates that Hydra can serve as a model for small molecule screens targeting the mechanosensory apparatus in native tissues.
Beschreibung:Gesehen am 09.02.2022
Beschreibung:Online Resource
ISSN:2045-2322
DOI:10.1038/s41598-021-99974-7

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