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: | , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
18 October 2021
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| 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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| 520 | |a 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. | ||
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