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  • Target = TRESK – 2 pore non-voltage gated potassium channel
  • Disease indication = Migraine (prevalent, debilitating and costly)
  • The potassium channel TRESK is abundant in trigeminal ganglia. The mutation causes loss of function, thereby increasing TG excitability. TRESK is therefore a viable therapeutic target for migraine
  • TRESK is activated strongly by second messengers such as calclum and volatile anaesthetics such as halothane
  • At resting membrane potential, channel is closed but activated by calcium. As a membrane depolarizes, potassium outflow through open TRESK channels tends to restore the membrane potential
  • Compound targeting TRESK and to increase TRESK opening in the resting state would reduce excitability and responsiveness
    Case Study – Hit Identification
  • Target was transiently expressed in U2OS cells using a Bacmam construct
  • FluxOR™ Potassium Ion Channel Assay in FLIPR Tetra
  • Selectivity required against TREK channel (heart) therefore selectivity assay developed
  • Almost all hits are TRESK specific

It's always satisfying when we are able to apply our expertise to a specific target class resulting in above average results.

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