Rapid microsome preparation from limited numbers of house flies

Wheelock, Geoffrey D.; Scott, Jeffrey G.

doi:10.1111/j.1570-7458.1991.tb01563.x

Cited by 5 publications

(1 citation statement)

References 13 publications

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“…A more modern approach towards studying insect enzymes in isolation, particularly those determined to be most important in the development of insecticide resistance, is the recombinant expression of enzymes using the tools of molecular biology. Since the 2002 discovery of the role that the Drosophila CYP450 CYP6G1 plays in metabolizing insecticides of multiple modes of action, the field has discovered that certain global insect pests have specific enzymes that are highly associated with the development of resistance . Now the testing of new experimental insecticides for stability in microsomes prepared from systems expressing recombinant enzymes that are associated with insecticide resistance is more common in discovery and development .…”

Section: Experimental Adme In Support Of Insecticide Discoverymentioning

confidence: 99%

Insecticide ADME for support of early‐phase discovery: combining classical and modern techniques

David

2016

Pest Management Science

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The two factors that determine an insecticide's potency are its binding to a target site (intrinsic activity) and the ability of its active form to reach the target site (bioavailability). Bioavailability is dictated by the compound's stability and transport kinetics, which are determined by both physical and biochemical characteristics. At BASF Global Insecticide Research, we characterize bioavailability in early research with an ADME (Absorption, Distribution, Metabolism and Excretion) approach, combining classical and modern techniques. For biochemical assessment of metabolism, we purify native insect enzymes using classical techniques, and recombinantly express individual insect enzymes that are known to be relevant in insecticide metabolism and resistance. For analytical characterization of an experimental insecticide and its metabolites, we conduct classical radiotracer translocation studies when a radiolabel is available. In discovery, where typically no radiolabel has been synthesized, we utilize modern high-resolution mass spectrometry to probe complex systems for the test compounds and its metabolites. By using these combined approaches, we can rapidly compare the ADME properties of sets of new experimental insecticides and aid in the design of structures with an improved potential to advance in the research pipeline. © 2016 Society of Chemical Industry.

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Section: Experimental Adme In Support Of Insecticide Discoverymentioning

confidence: 99%