Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans

@article{Cully1994CloningOA,
  title={Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans},
  author={Doris F. Cully and Demetrios K. Vassilatis and Ken K. Liu and Philip S. Paress and Lex H. T. Van der Ploeg and James M. Schaeffer and Joseph P. Arena},
  journal={Nature},
  year={1994},
  volume={371},
  pages={707-711}
}
THE avermectins are a family of macrocyclic lactones used in the control of nematode and arthropod parasites1. Ivermectin (22,23-dihydroavermectin Bla) is widely used as an anthelmintic in veterinary medicine and is used to treat onchocerciasis or river blindness in humans1,2. Abamectin (avermectin B1a) is a miticide and insecticide used in crop protection1. Avermectins interact with vertebrate and invertebrate GABA receptors3–7 and invertebrate glutamate-gated chloride channels8–11. The soil… 
Genetic and Biochemical Evidence for a Novel Avermectin-sensitive Chloride Channel in Caenorhabditis elegans
TLDR
Avermectins are a class of macrocyclic lactones that is widely used in crop protection and to treat helminth infections in man and animals and the presence of subunits related to GluClα may explain the low level and rarity of target site involvement in resistance to the avermectin class of compounds.
Identification of a Drosophila melanogaster Glutamate-gated Chloride Channel Sensitive to the Antiparasitic Agent Avermectin*
TLDR
The pharmacological data support the hypothesis that the DrosGluCl-α channel represents the arthropod H-receptor and an important target for the avermectin class of insecticides.
Identification and Functional Expression of a Glutamate- and Avermectin-Gated Chloride Channel from Caligus rogercresseyi, a Southern Hemisphere Sea Louse Affecting Farmed Fish
TLDR
It is suggested that CrGluClα is an important target for avermectins used in the treatment of sea louse infestation in farmed salmonids and open the way for ascertaining a possible mechanism of increasing resistance to MLs in aquaculture industry.
Correction: Identification and Functional Expression of a Glutamate- and Avermectin-Gated Chloride Channel from Caligus rogercresseyi, a Southern Hemisphere Sea Louse Affecting Farmed Fish
TLDR
It is suggested that CrGluCla is an important target for avermectins used in the treatment of sea louse infestation in farmed salmonids and open the way for ascertaining a possible mechanism of increasing resistance to MLs in aquaculture industry.
An Ivermectin-Sensitive Glutamate-Gated Chloride Channel from the Parasitic Nematode Haemonchus contortus
TLDR
Molecular modeling studies suggested that the GluCl subunits have a fold similar to that of other Cys-loop ligand-gated ion channels and that amino acid 256 was unlikely to play a direct role in ligand binding but may be involved in mediating the allosteric properties of the receptor.
Characterisation of glutamate-gated chloride channels from Caenorhabditis elegans.
TLDR
R reverse transcriptase-polymerase chain reaction techniques are used to isolate cDNAs encoding the products o f the gbr-2/avr-14 orthologues from the parasitic nematodes Haemonchus contortus and Ascaris suum, and predicted polypeptides possess all the characteristics of the ligand-gated chloride channels.
Evolutionary Relationship of the Ligand-Gated Ion Channels and the Avermectin-Sensitive, Glutamate-Gated Chloride Channels
TLDR
The gene structure and phylogenetic analyses in combination with the distinct pharmacological properties demonstrate that GluClα and Glu cloned genes belong to a discrete ligand-gated ion channel family that may represent genes orthologous to the vertebrate glycine channels.
Glutamate-gated chloride channels and the mode of action of the avermectin/milbemycin anthelmintics
TLDR
The known expression patterns of the GluCl explain most of the observed biological effects of treatment with the macrocyclic lactones, though the reason for the long-lasting inhibition of larval production in filarial species is still poorly understood.
Drug-resistant Drosophila indicate glutamate-gated chloride channels are targets for the antiparasitics nodulisporic acid and ivermectin.
TLDR
Genetics and sequencing identified a proline to serine mutation (P299S) in the gene coding for the glutamate-gated chloride channel subunit DmGluClalpha, providing direct evidence that nodulisporic acid and ivermectin act on DmgluCl alpha channels.
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TLDR
The proteins that were covalently tagged in these experiments are believed to be associated with avermectin-sensitive chloride channels present in the neuromuscular systems of C. elegans and D. melanogaster.
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