Development of a novel screening system to identify activators to two-pore domain potassium channels (K2Ps)


ICMS 2018 UK


David McCoull, Emma Ococks, Paul D Wright



K2P channels are characterised by their four transmembrane
domain, two-pore topology. Sub-units dimerise to form a
functional channel.

K2P channels carry background (or leak) potassium current in
a variety of cell types and primarily act to maintain resting
membrane potential.

Despite a number of important roles they have proved a
difficult target class to modulate with small molecules.

Thus, there is currently a lack of useful specific
pharmacological tools which target K2Ps. This has limited the
interrogation of the precise physiological function of K2Ps and
efforts to generate K2P targeting therapeutics.

K2Ps have been implicated in a number of human
pathophysiologies including, but not limited to, pain (TREK-1,
TREK-2, TRAAK), migraine (TRESK), Birk-Barel syndrome
(TASK-3) and Balkan endemic nephropathy (TASK-2).

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