Understanding ion channel inhibition to open doors in drug discovery

Scientists have discovered how drug-like small molecules can regulate the activity of therapeutically relevant ion channels – and their findings could transform ongoing drug development efforts.

The new study provides detailed insight into the regulation of TRPC5 ion channels, which allow positively charged ions such as calcium, sodium and potassium to flow in and out of cells.

TRPC5 channels are considered potential therapeutic targets for the treatment of a range of conditions, including anxiety, kidney disease and cardiovascular disease.

Led by Dr Robin Bon, Associate Professor of Chemical Biology in the School of Medicine, and Dr Stephen Muench, Associate Professor of Membrane Biology in the School of Biomedical Sciences, and both members of the Astbury Centre for Structural Molecular Biology, the study reveals how a drug-like small molecule, called Pico145, binds to the TRPC5 channel, thereby preventing the channel from opening.

Read the full press release on the Faculty of Biological Sciences website

Read Cryo-EM structures of human TRPC5 reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding siteĀ on the Communications Biology website