Dawn Wong - Towards a Species-Selective Acetylcholinesterase Inhibitor to Control the Mosquito Vector of Malaria, Anopheles gambiae

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      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.

      http://dx.doi.org/10.1016/j.cbi.2008.04.037

     

      Abstract:

      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