|
Background
|
Tertiapin has been isolated from the venom of the Honeybee Apis mellifera (African tarantula). Tertiapin-Q is a mutant of tertiapin where M13 has been mutated by Q in order to increase your stability. This is a neurotoxin with presynaptic activity that blocks the inwardly rectifying Kir1.1 (KCNJ1) and Kir3.1/3.4 (KCNJ3/KCNJ5) potassium channels with high affinity by binding to the M1-M2 linker region of thesechannels in a 1:1 stoichiometry. Tertiapin-Q also inhibits calcium-activated large conductance BK-type (KCNMA/KCNMB) potassium channels in a concentration, and voltage-dependent manner, in addition to inhibiting Kir3.1/3.2 (KCNJ3/KCNJ6) heteromultimer potassiumchannels.
|
