A molecular characterization of the agonist binding site of a nematode cys-loop GABA receptor.

ABSTRACT:

Background and purpose

Cys-loop GABA receptors represent important targets for human chemotherapeutics and insecticides and are potential targets for novel anthelmintics (nematicides). However, compared with insect and mammalian receptors, little is known regarding the pharmacological characteristics of nematode Cys-loop GABA receptors. Here we have investigated the agonist binding site of the Cys-loop GABA receptor UNC-49 (Hco-UNC-49) from the parasitic nematode Haemonchus contortus.

Experimental approach

We used two-electrode voltage-clamp electrophysiology to measure channel activation by classical GABA receptor agonists on Hco-UNC-49 expressed in Xenopus laevis oocytes, along with site-directed mutagenesis and in silico homology modelling.

Key results

The sulphona

SUBMITTER: Kaji MD 

PROVIDER: S-EPMC4523332 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature