Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Presynaptic neurotoxin 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 these channels in a 1:1 stoichiometry. It may block the potassium channel pore by occluding its alpha helix into the channel vestibule. Tertiapin-Q also inhibits calcium-activated large conductance BK-type (KCNMA) potassium channels in a concentration-, and voltage-dependent manner, in addition to inhibiting Kir3.1/3.2 (KCNJ3/KCNJ6) heteromultimers potassium channels. It can prevent dose-dependently acetylcholine(ACh)-induced atrioventricular blocks in mammalian hearts, as KCNJ3/KCNJ5 channels (also named I(KACh), because these channels are activated by ACh) are found in mammalian myocytes. Interacts specifically with calmodulin in the presence of calcium. {ECO:0000269|PubMed:10572004, ECO:0000269|PubMed:10734170, ECO:0000269|PubMed:11015309, ECO:0000269|PubMed:16725344, ECO:0000269|PubMed:6091685, ECO:0000269|PubMed:9748337}.
Target
voltage-gated potassium channel (Kv)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Apis mellifera (Honeybee)
Neurotoxin
Presynaptic neurotoxin
Calcium-activated potassium channel impairing toxin
Ion channel impairing toxin
Potassium channel impairing toxin
Presynaptic neurotoxin 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 these channels in a 1:1 stoichiometry. It may block the potassium channel pore by occluding its alpha helix into the channel vestibule.
Tertiapin (TPN)
insect
Evidence at protein level
3D-structure
Calcium-activated potassium channel impairing toxin
Calmodulin-binding
Direct protein sequencing
Disulfide bond
Ion channel impairing toxin
Neurotoxin
Oxidation
Potassium channel impairing toxin
Presynaptic neurotoxin
Reference proteome
Secreted
Toxin
TISSUE SPECIFICITY: Expressed by the venom gland. {ECO:0000305|PubMed:9748337, ECO:0000305|Ref.1}.