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Hofmann D, Garg N, Grässle S, et al. A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra. Sci Rep. 2021;11(1):20627doi: 10.1038/s41598-021-99974-7.
Hofmann, D., Garg, N., Grässle, S., Vanderheiden, S., Bergheim, B. G., Bräse, S., Jung, N., & Özbek, S. (2021). A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra. Scientific reports, 11(1), 20627. https://doi.org/10.1038/s41598-021-99974-7
Hofmann, Diana, et al. "A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra." Scientific reports vol. 11,1 (2021): 20627. doi: https://doi.org/10.1038/s41598-021-99974-7
Hofmann D, Garg N, Grässle S, Vanderheiden S, Bergheim BG, Bräse S, Jung N, Özbek S. A small molecule screen identifies novel inhibitors of mechanosensory nematocyst discharge in Hydra. Sci Rep. 2021 Oct 18;11(1):20627. doi: 10.1038/s41598-021-99974-7. PMID: 34663887; PMCID: PMC8523708.
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Sci Rep. 2021 Oct 18;11(1):20627. doi: 10.1038/s41598-021-99974-7.

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

Scientific reports

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

Affiliations

  1. Department of Molecular Evolution and Genomics, Centre for Organismal Studies, University of Heidelberg, Im Neuenheimer Feld 230, 69120, Heidelberg, Germany.
  2. Karlsruhe Institute of Technology, Institute of Biological and Chemical Systems - Functional Molecular Systems (IBCS-FMS), Hermann-von-Helmholtz Platz 1, 76344, Eggenstein-Leopoldshafen, Germany.
  3. Karlsruhe Institute of Technology, Institute of Organic Chemistry, Fritz-Haber-Weg 6, 76131, Karlsruhe, Germany.
  4. Karlsruhe Institute of Technology, Institute of Biological and Chemical Systems - Functional Molecular Systems (IBCS-FMS), Hermann-von-Helmholtz Platz 1, 76344, Eggenstein-Leopoldshafen, Germany. [email protected].
  5. Karlsruhe Institute of Technology, Institute of Organic Chemistry, Fritz-Haber-Weg 6, 76131, Karlsruhe, Germany. [email protected].
  6. Department of Molecular Evolution and Genomics, Centre for Organismal Studies, University of Heidelberg, Im Neuenheimer Feld 230, 69120, Heidelberg, Germany. [email protected].

PMID: 34663887 PMCID: PMC8523708 DOI: 10.1038/s41598-021-99974-7

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.

© 2021. The Author(s).

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