G protein coupled receptors (GPCRs) are a major target for drug discovery. Estimates in the literature are that somewhere between 30 and 60% of all drugs in use target these receptors. Of the human genome, about 4% of all proteins encoded are GPCRs. There are around 800 known human GPCRs, although many of these are olfactory receptors. All biogenic amine and most peptide hormone receptors are GPCRs. A huge number of drugs are agonist or antagonists of biogenic amines. Antagonists of corticotropin-releasing factor are under development for a variety of conditions; calcitonin is used for treating osteoporosis. This includes many of the best selling drugs, including histamine H1 and H2 receptors, a and � adrenergic receptor agonists and antagonists, etc. Fifty-six human GPCRs are drug targets. Yet to date, the only insect GPCR which is a target of a pesticide is the dopamine receptor, of which chlordimeform is the prototypical receptor agonist. Most vital life functions in insects are controlled by GPCRs presenting a huge number of possibilities for development of new selective insecticides. I will review the structure, function, and action of GPCRs.

G protein coupled receptors as targets for insecticide discovery

246th National Meeting (2013)

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