The Emerging Structural Pharmacology of ATP-Sensitive Potassium Channels
September 2022
in “
Molecular pharmacology
”
TLDR KATP channels are important for energy balance and are targeted by drugs for diabetes, hypoglycemia, hypertension, and hair loss.
ATP-sensitive potassium channels (KATP) are crucial for energy homeostasis and are involved in various physiological processes. They are significant drug targets, with KATP inhibitors used for diabetes and KATP activators for hypoglycemia, hypertension, and hair loss. Recent cryogenic electron microscopy studies have revealed the drug binding modes, showing that inhibitors and activators bind to distinct sites in the transmembrane domain of the sulfonylurea receptor (SUR) subunit. These studies also suggest that these drugs may allosterically modulate the dimerization of SUR nucleotide-binding domains (NBDs), thereby affecting KATP channel activity.
