Overproduction of a P450 that metabolizes diazinon is linked to a loss‐of‐function in the chromosome 2 ali‐esterase (<i>MdαE7</i>) gene in resistant house flies

Sabourault, Cécile; Guzov, Victor M.; Koener, J. F.; Claudianos, Charles; Plapp, Frederick W.; Feyereisen, René

doi:10.1046/j.0962-1075.2001.00303.x

Cited by 84 publications

(44 citation statements)

References 60 publications

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“…It was suggested that the same regulatory (trans-acting) gene may be involved in both induction and biochemical resistance (Terriere, 1983), and Plapp (1984) further proposed that a receptor involved in xenobiotic induction may be altered in resistant insects. However, despite growing evidence that overexpression of some P450 genes in resistant strains can involve trans-regulating factors (e.g., Sabourault et al, 2001), a link with induction has remained tenuous. Genetic analysis in Drosophila indicates that expressions of Cyp6a2 and Cyp6a8 are controlled in trans by a negative regulator (Dombrowski et al, 1998;Maitra et al, 2000 andMaitra et al, 2002).…”

Section: Discussionmentioning

confidence: 99%

Xenobiotic response in Drosophila melanogaster: Sex dependence of P450 and GST gene induction

Goff

Hilliou

Siegfried

et al. 2006

Insect Biochemistry and Molecular Biology

146

109

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Section: Discussionmentioning

confidence: 99%

Xenobiotic response in Drosophila melanogaster: Sex dependence of P450 and GST gene induction

Goff

Hilliou

Siegfried

et al. 2006

Insect Biochemistry and Molecular Biology

146

109

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“…Although higher expression in insecticide-resistant strains does not necessarily guarantee relevance to insecticide resistance (12), CYP6Z1 has been repeatedly highlighted as overexpressed in adult males and females of the permethrin-resistant RSP strain collected in West Kenya (East Africa) and constitutively expressed at low levels in larvae and pupae of the RSP strain (13,14). And CYP6Z2 (but not CYP6Z1) has been documented as overexpressed in adult males and females of the permethrin-resistant Odumasy strain collected in Southern Ghana (West Africa) (15).Noting that DDT-metabolizing and cypermethrin-metabolizing P450s have already been identified in the CYP6 family of dipterans (Drosophila melanogaster and Musca domestica) and lepidopterans (Helicoverpa zea) (16)(17)(18)(19)(20)(21)(22), the overall purpose of this study was to determine whether any of CYP6 family transcripts expressed at higher levels in DDT-resistant strains have potential to code for a P450 capable of metabolizing DDT. Because we were specifically interested in comparing the metabolic profiles of the closely related CYP6Z1 and CYP6Z2 (69.6% amino acid identity), molecular modelings were carried out to predict their catalytic site geometries.…”

mentioning

confidence: 99%

“…Noting that DDT-metabolizing and cypermethrin-metabolizing P450s have already been identified in the CYP6 family of dipterans (Drosophila melanogaster and Musca domestica) and lepidopterans (Helicoverpa zea) (16)(17)(18)(19)(20)(21)(22), the overall purpose of this study was to determine whether any of CYP6 family transcripts expressed at higher levels in DDT-resistant strains have potential to code for a P450 capable of metabolizing DDT. Because we were specifically interested in comparing the metabolic profiles of the closely related CYP6Z1 and CYP6Z2 (69.6% amino acid identity), molecular modelings were carried out to predict their catalytic site geometries.…”

mentioning

confidence: 99%

Comparative molecular modeling of Anopheles gambiae CYP6Z1, a mosquito P450 capable of metabolizing DDT

Chiu

Wen

Rupasinghe

et al. 2008

Proc. Natl. Acad. Sci. U.S.A.

164

138

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One of the challenges faced in malarial control is the acquisition of insecticide resistance that has developed in mosquitoes that are vectors for this disease. Anopheles gambiae, which has been the major mosquito vector of the malaria parasite Plasmodium falciparum in Africa, has over the years developed resistance to insecticides including dieldrin, 1,1-bis(p-chlorophenyl)-2,2,2-trichloroethane (DDT), and pyrethroids. Previous microarray studies using fragments of 230 An. gambiae genes identified five P450 loci, including CYP4C27, CYP4H15, CYP6Z1, CYP6Z2, and CYP12F1, that showed significantly higher expression in the DDT-resistant ZAN/U strain compared with the DDT-susceptible Kisumu strain. To predict whether either of the CYP6Z1 and CYP6Z2 proteins might potentially metabolize DDT, we generated and compared molecular models of these two proteins with and without DDT docked in their catalytic sites. This comparison indicated that, although these two CYP6Z proteins share high sequence identity, their metabolic profiles were likely to differ dramatically from the larger catalytic site of CYP6Z1, potentially involved in DDT metabolism, and the more constrained catalytic site of CYP6Z2, not likely to metabolize DDT. Heterologous expressions of these proteins have corroborated these predictions: only CYP6Z1 is capable of metabolizing DDT. Overlays of these models indicate that slight differences in the backbone of SRS1 and variations of side chains in SRS2 and SRS4 account for the significant differences in their catalytic site volumes and DDT-metabolic capacities. These data identify CYP6Z1 as one important target for inhibitor design aimed at inactivating insecticide-metabolizing P450s in natural populations of this malarial mosquito.cytochrome P450 monooxygenases ͉ insecticides ͉ plant allelochemicals I n 2004, the World Health Organization reported that up to 2.7 million people die of malaria every year with 80-90% of these deaths occurring in Africa (ref. 1 and www.africanfront.com/ AIDS1.php). Many prevention and treatment strategies have been developed to tackle this life-threatening disease from the side of the mosquito vector and that of the human host (2, 3). These range from antimalarial drugs to indoor spraying of insecticides and use of bed nets treated with pyrethroid insecticides. Although these practices have helped reduce human mortality, various issues have emerged with mosquito vectors developing insecticide resistance and parasites developing drug resistance. Both of these significantly reduce the efficacy of current malarial prevention and treatment practices (2, 4-8).The development of insecticide resistance in mosquito vectors is illustrated by Anopheles gambiae, which has been the major mosquito vector of the malaria parasite Plasmodium falciparum in Africa (4, 6). Throughout the years, people have reported Anopheles resistance (albeit low-level resistance) to various insecticides including dieldrin (a cyclodiene-type insecticide), 1,1-bis(pchlorophenyl)-2,2,2-trichloroethane (DDT), and pe...

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“…According to this hypothesis, at 2%, the effects of isomers responsible for the bioactivation of TE increased, offsetting the effect of the isomers involved in metabolic detoxifi cation [18][19][20][21][22] .…”

Section: Effects Of Pbo On Esterase Activitymentioning

confidence: 99%

Effects of piperonyl butoxide on the toxicity of the organophosphate temephos and the role of esterases in the insecticide resistance of Aedes aegypti

Pereira

Limongi

Júnior

et al. 2014

Rev. Soc. Bras. Med. Trop.

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Introduction: The effects of piperonyl butoxide (PBO) on the toxicity of the organophosphate temephos (TE) and the role of esterases in the resistance of Aedes aegypti to this insecticide were evaluated. Methods: A. aegypti L4 larvae susceptible and resistant to TE were pre-treated with PBO solutions in acetone at concentrations of 0.125, 0.25, 0.5, 1, and 2% for 24h and subsequently exposed to a diagnostic concentration of 0.02mg/L aqueous TE solution. The esterase activity of the larvae extracts pre-treated with varying PBO concentrations and exposed to TE for three time periods was determined. Results: At concentrations of 0.25, 0.5, 1, and 2%, PBO showed a signifi cant synergistic effect with TE toxicity. High levels of esterase activity were associated with the survival of A. aegypti L4 larvae exposed to TE only. Conclusions: The results of the biochemical assays suggest that PBO has a signifi cant inhibitory effect on the total esterase activity in A. aegypti larvae.Keywords: Temephos. Insecticide resistance. Aedes aegypti. Esterases.Dengue fever, a major viral disease, is a serious public health problem, especially in tropical countries where the climate and urban culture provide optimal conditions for the development and proliferation of its main vector, the mosquito Aedes aegypti 1 . The control of A. aegypti is primarily based on the use of chemical and biological products that are integrated with environmental management programs. Public programs aimed at controlling mosquitoes are characterized by the use of commercial insecticides, including organophosphates and pyrethroids. The organophosphate temephos (TE) was widely used in Brazil to control A. aegypti larvae until recently; however, due to reports of vector resistance to this insecticide, this method was replaced by the National Dengue Control Program. Nevertheless, TE remains on the list of insecticides to control dengue in Brazil and may be used again in the future 2,3 .The resistance to insecticides has contributed to an increase in A. aegypti populations and the incidence of dengue cases in Asia, and Central and South America, especially in Brazil 2,4 .The biochemical mechanisms involved in the development of resistance to insecticides include detoxifi cation metabolism processes. Several enzymes and enzyme systems participate in these processes, including oxidases, esterases, and transferases 5 . These enzymes allow the insect to convert an insecticide to a nontoxic form or to rapidly eliminate the compound from the body.Synergists such as piperonyl butoxide (PBO) have been employed in an attempt to overcome resistance to insecticides. Synergists are known to act as an alternative substrate, competing with the insecticide and interfering with detoxification. Synergists also act allosterically to inhibit the binding sites of esterases and multifunction oxidases (MFOs), minimizing the amount of insecticide needed to control insects and the levels of environmental contamination by pesticide residues 6 .Several studies have demonstrate...

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Overproduction of a P450 that metabolizes diazinon is linked to a loss‐of‐function in the chromosome 2 ali‐esterase (MdαE7) gene in resistant house flies

Cited by 84 publications

References 60 publications

Xenobiotic response in Drosophila melanogaster: Sex dependence of P450 and GST gene induction

Xenobiotic response in Drosophila melanogaster: Sex dependence of P450 and GST gene induction

Comparative molecular modeling of Anopheles gambiae CYP6Z1, a mosquito P450 capable of metabolizing DDT

Effects of piperonyl butoxide on the toxicity of the organophosphate temephos and the role of esterases in the insecticide resistance of Aedes aegypti

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