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Mechanisms of action of emodepside

Mechanisms of action of emodepside
Mechanisms of action of emodepside
The research of the class of cyclic octadepsipeptides started at the beginning of the 1990s. PF1022A, the starting material of emodepside, is a natural secondary metabolite of the fungus Mycelia sterilia, which belongs to the microflora of the leaves of Camellia japonica. PF1022A consists of four N-methyl-L-leucins, two D-Iactic acids and two D-phenyllactic acids, which build up a cyclic octadepsipeptide with an alternating L-D-L-configuration. Emodepside is a semisynthetic derivative of PF1022A, which contains a morpholine attached in para position at each of both D-phenyllactic acids. Emodepside is efficacious against a variety of gastrointestinal nematodes. Emodepside binds to a presynaptic latrophilin receptor in nematodes. The following presynaptic signal transduction occurs via activation of Gqalpha protein and phospholipase-Cbeta, which leads to mobilization of diacylglycerol (DAG). DAG then activates UNC-13 and synaptobrevin, two proteins which play an important role in presynaptic vesicle-functioning. This finally leads to the release of a currently unidentified transmitter. The transmitter (or modulator) exerts its effects at the postsynaptic membrane and induces a flaccid paralysis of the pharynx and the somatic musculature in nematodes.
0932-0113
S1-S10
Harder, A.
0cf8ea99-09fd-416c-ab07-4c7f4d63d44c
Holden–Dye, L.
9511bcd1-d6eb-491b-9873-424c4779c0b9
Walker, R.
9368ac2d-f1e9-4bd9-a4b4-4a161c4aa140
Wunderlich, F.
403a3900-810d-42cd-be72-479f39af29bd
Harder, A.
0cf8ea99-09fd-416c-ab07-4c7f4d63d44c
Holden–Dye, L.
9511bcd1-d6eb-491b-9873-424c4779c0b9
Walker, R.
9368ac2d-f1e9-4bd9-a4b4-4a161c4aa140
Wunderlich, F.
403a3900-810d-42cd-be72-479f39af29bd

Harder, A., Holden–Dye, L., Walker, R. and Wunderlich, F. (2005) Mechanisms of action of emodepside. Parasitology Research, 97, supplement 1, S1-S10. (doi:10.1007/s00436-005-1438-z). (PMID:16228263)

Record type: Article

Abstract

The research of the class of cyclic octadepsipeptides started at the beginning of the 1990s. PF1022A, the starting material of emodepside, is a natural secondary metabolite of the fungus Mycelia sterilia, which belongs to the microflora of the leaves of Camellia japonica. PF1022A consists of four N-methyl-L-leucins, two D-Iactic acids and two D-phenyllactic acids, which build up a cyclic octadepsipeptide with an alternating L-D-L-configuration. Emodepside is a semisynthetic derivative of PF1022A, which contains a morpholine attached in para position at each of both D-phenyllactic acids. Emodepside is efficacious against a variety of gastrointestinal nematodes. Emodepside binds to a presynaptic latrophilin receptor in nematodes. The following presynaptic signal transduction occurs via activation of Gqalpha protein and phospholipase-Cbeta, which leads to mobilization of diacylglycerol (DAG). DAG then activates UNC-13 and synaptobrevin, two proteins which play an important role in presynaptic vesicle-functioning. This finally leads to the release of a currently unidentified transmitter. The transmitter (or modulator) exerts its effects at the postsynaptic membrane and induces a flaccid paralysis of the pharynx and the somatic musculature in nematodes.

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More information

Published date: October 2005
Organisations: Centre for Biological Sciences

Identifiers

Local EPrints ID: 372593
URI: http://eprints.soton.ac.uk/id/eprint/372593
ISSN: 0932-0113
PURE UUID: 1018bdd9-b8a0-4f65-a91e-a30d5b96ad09
ORCID for R. Walker: ORCID iD orcid.org/0000-0002-9031-7671

Catalogue record

Date deposited: 09 Dec 2014 13:47
Last modified: 10 Dec 2019 01:23

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