Historically, ion channels have been the most successful insecticidal targets, and therefore have been the focus of our target-based approach for novel insecticidal entities. From the roughly 15000 insect genes, 150 are ion channels, and from this we identified a subset of potential insecticidal targets. Several potassium channels were identified as potentially lethal targets and were selected for cloning and expression in mammalian cell lines. High throughput screens on an internal library yielded a number of hits in the micromolar activity range. This approach was exemplified by our work on the calcium-activated potassium channels Sk and Slack. A chemical synthesis program allowed us to optimize the identified hit series, resulting in compounds with activity in the low nanomolar range. We will discuss our screening process, the chemical optimization of this hit class, and the value of potassium channels as insecticidal targets.

Potassium channels as insecticidal targets

244th National Meeting (2012)

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