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Emodepside, a cyclo-octadepsipeptide anthelmintic with a novel mode of action

Emodepside, a cyclo-octadepsipeptide anthelmintic with a novel mode of action
Emodepside, a cyclo-octadepsipeptide anthelmintic with a novel mode of action
Due to the development of drug resistance, there is a continual need for new anthelmintics with novel modes of action. Emodepside, a cyclo-octadepsipeptide, was originally thought to modify GABAergic transmission in parasitic nematodes. However, more recent studies using the parasitic nematode Ascaris suum and the free-living nematode Caenorhabditis elegans indicate that emodepside interacts with a presynaptic latrophilin receptor to release a transmitter or modulator. This presynaptic signaling pathway involves activation of a Gaq protein and phospholipase-?, which mobilizes diacylglycerol (DAG). DAG activates UNC-13, which in turn activates synaptobrevin to increase release of the transmitter or modulator. The released transmitter or modulator acts postsynaptically to modify pharyngeal and somatic body wall muscle activity.
0377-8282
1015-1024
Amliwala, K.
e71463eb-6480-4395-8e2a-57a005809be8
Bull, K.
a9291d1b-339f-4b4c-a510-17de496d96be
Willson, J.
3fe4cbeb-fd6f-4e81-af4f-3b753e358e5c
Harder, A.
0cf8ea99-09fd-416c-ab07-4c7f4d63d44c
Holden-Dye, L.
8032bf60-5db6-40cb-b71c-ddda9d212c8e
Walker, R.J.
b6597591-587e-488a-8a54-89156c42ce8d
Amliwala, K.
e71463eb-6480-4395-8e2a-57a005809be8
Bull, K.
a9291d1b-339f-4b4c-a510-17de496d96be
Willson, J.
3fe4cbeb-fd6f-4e81-af4f-3b753e358e5c
Harder, A.
0cf8ea99-09fd-416c-ab07-4c7f4d63d44c
Holden-Dye, L.
8032bf60-5db6-40cb-b71c-ddda9d212c8e
Walker, R.J.
b6597591-587e-488a-8a54-89156c42ce8d

Amliwala, K., Bull, K., Willson, J., Harder, A., Holden-Dye, L. and Walker, R.J. (2004) Emodepside, a cyclo-octadepsipeptide anthelmintic with a novel mode of action. Drugs of the Future, 29 (10), 1015-1024. (doi:10.1358/dof.2004.029.10.863392).

Record type: Article

Abstract

Due to the development of drug resistance, there is a continual need for new anthelmintics with novel modes of action. Emodepside, a cyclo-octadepsipeptide, was originally thought to modify GABAergic transmission in parasitic nematodes. However, more recent studies using the parasitic nematode Ascaris suum and the free-living nematode Caenorhabditis elegans indicate that emodepside interacts with a presynaptic latrophilin receptor to release a transmitter or modulator. This presynaptic signaling pathway involves activation of a Gaq protein and phospholipase-?, which mobilizes diacylglycerol (DAG). DAG activates UNC-13, which in turn activates synaptobrevin to increase release of the transmitter or modulator. The released transmitter or modulator acts postsynaptically to modify pharyngeal and somatic body wall muscle activity.

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More information

Published date: 1 October 2004

Identifiers

Local EPrints ID: 56661
URI: http://eprints.soton.ac.uk/id/eprint/56661
ISSN: 0377-8282
PURE UUID: fac69b71-5616-4abb-a794-068164f8ed47
ORCID for L. Holden-Dye: ORCID iD orcid.org/0000-0002-9704-1217

Catalogue record

Date deposited: 08 Aug 2008
Last modified: 18 Feb 2021 16:34

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