Publication Details (including relevant citation information):
Carlier, P. R.; Anderson, T. D.; Wong, D. M.; Hsu, D. C.; Hartsel, J.; Ma, M.; Wong, E. A.; Choudhury, R.; Lam, P. C.-H.; Totrov, M. M.; Bloomquist, J. R. Towards a Species-Selective Acetylcholinesterase Inhibitor to Control the Mosquito Vector of Malaria, Anopheles gambiae. Chemico-Biological Interactions 2008, 175, 368-375. PMID: 18554580.
Anopheles gambiae is themajor mosquito vector of malaria in sub-Saharan Africa. At present, insecticide-treated nets (ITNs) impregnated with pyrethroid insecticides are widely used in malaria-endemic regions to reduce infection; however the emergence of pyrethroidresistant mosquitoes has significantly reduced the effectiveness of the pyrethroid ITNs. An acetylcholinesterase (AChE) inhibitor that is potent for An. gambiae but weakly potent for the human enzyme could potentially be safely deployed on a new class of ITNs. In this paper we provide a preliminary pharmacological characterization of An. gambiae AChE, discuss structural features of An. gambiae and human AChE that could lead to selective inhibition, and describecompounds with 130-fold selectivity for inhibition of An. gambiae AChE relative to human AChE.
Address (URL): http://dx.doi.org/10.1016/j.cbi.2008.04.037