Abstract：
:Anopheles gambiae is the major 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 pyrethroid-resistant 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 describe compounds with 130-fold selectivity for inhibition of An. gambiae AChE relative to human AChE.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Carlier PR,Anderson TD,Wong DM,Hsu DC,Hartsel J,Ma M,Wong EA,Choudhury R,Lam PC,Totrov MM,Bloomquist JRdoi
10.1016/j.cbi.2008.04.037subject
Has Abstractpub_date
2008-09-25 00:00:00pages
368-75issue
1-3eissn
0009-2797issn
1872-7786pii
S0009-2797(08)00245-7journal_volume
175pub_type
杂志文章abstract：:The formation and disappearance of DNA single-strand breaks (SSB) produced by 4-demethoxydaunorubicin (4-dmDR) in P388 murine leukemia cells and in a resistant subline were examined by alkaline elution methods in relation to cellular pharmacokinetics. DNA strand breaks produced by this intercalating agent were essenti...
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
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journal_title：Chemico-biological interactions
pub_type： 杂志文章
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更新日期：2016-06-25 00:00:00
