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

Hofmann, Diana; Garg, Niharika; Grässle, Simone; Vanderheiden, Sylvia; Bergheim, Bruno Gideon; Bräse, Stefan; Jung, Nicole; Özbek, Suat

Abstract:

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.


Verlagsausgabe §
DOI: 10.5445/IR/1000142532
Veröffentlicht am 28.01.2022
Originalveröffentlichung
DOI: 10.1038/s41598-021-99974-7
Scopus
Zitationen: 1
Dimensions
Zitationen: 4
Cover der Publikation
Zugehörige Institution(en) am KIT Institut für Biologische und Chemische Systeme (IBCS)
Institut für Organische Chemie (IOC)
Publikationstyp Zeitschriftenaufsatz
Publikationsjahr 2021
Sprache Englisch
Identifikator ISSN: 2045-2322
KITopen-ID: 1000142532
HGF-Programm 43.33.11 (POF IV, LK 01) Adaptive and Bioinstructive Materials Systems
Erschienen in Scientific reports
Verlag Nature Research
Band 11
Seiten Art.-Nr. 20627
Vorab online veröffentlicht am 18.10.2021
Nachgewiesen in Scopus
Web of Science
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