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TMEM16A - a robust high throughput e-phys assay for a key ion channel involved in cancer and cystic fibrosis

News   •   Nov 28, 2016 12:57 GMT

TMEM16A is a hot therapeutic target. Activation of TMEM16A with pharmacological compounds could bypass the primary defect in Cystic Fibrosis. Also inhibition of TMEM16A has been suggested to suppress tumor growth and invasion in human lung and colorectal cancer.... among others.

At Sophion we recently developed a novel approach to assay pharmacological modulation of TMEM16A on Qube with precisely clamped internal Ca2+ and high seal resistances throughout the entire experiment.

  • Consistently high success rates ( >80%)
  • High degree of pharmacological reproducibility
  • Very low run down and data spread

A robust TMEM16A assay for automated patch clamp has long been awaited but progress has been hampered as many automated patch clamp devices rely on the use of fluoride in the internal solution.

Fluoride exhibits a very low solubility with calcium which means that calcium that is added to the internal solution to activate the channel has a strong tendency to precipitate, making it impossible to correctly adjust the calcium concentration.

We expect that our novel approach in assay design for Qube384 will be applicable to other calcium activated channels (SK, BK, IK, TRPC1 etc.), so they can be performed with the same high success rates, reproducibility and accuracy.

You can download the application report here

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