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Ссылка на источник |
Scorpion toxins interact with nicotinic acetylcholine receptors
|
01.10.2019 |
Kasheverov I.
Oparin P.
Zhmak M.
Egorova N.
Ivanov I.
Gigolaev A.
Nekrasova O.
Serebryakova M.
Kudryavtsev D.
Prokopev N.
Hoang A.
Tsetlin V.
Vassilevski A.
Utkin Y.
|
FEBS Letters |
10.1002/1873-3468.13530 |
1 |
Ссылка
© 2019 Federation of European Biochemical Societies Neurotoxins are among the main components of scorpion and snake venoms. Scorpion neurotoxins affect voltage-gated ion channels, while most snake neurotoxins target ligand-gated ion channels, mainly nicotinic acetylcholine receptors (nAChRs). We report that scorpion venoms inhibit α-bungarotoxin binding to both muscle-type nAChR from Torpedo californica and neuronal human α7 nAChR. Toxins inhibiting nAChRs were identified as OSK-1 (α-KTx family) from Orthochirus scrobiculosus and HelaTx1 (κ-KTx family) from Heterometrus laoticus, both being blockers of voltage-gated potassium channels. With an IC50 of 1.6 μm, OSK1 inhibits acetylcholine-induced current through mouse muscle-type nAChR heterologously expressed in Xenopus oocytes. Other well-characterized scorpion toxins from these families also bind to Torpedo nAChR with micromolar affinities. Our results indicate that scorpion neurotoxins present target promiscuity.
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