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Open AccessArticle

Novel Three-Finger Neurotoxins from Naja melanoleuca Cobra Venom Interact with GABAA and Nicotinic Acetylcholine Receptors

1
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, ul. Miklukho-Maklaya 16/10, 117997 Moscow, Russia
2
Moscow Institute of Physics and Technology, 141700 Dolgoprudny, Russia
3
Institute of Molecular Medicine, Sechenov First Moscow State Medical University, ul. Trubetskaya 8, bld. 2, 119991 Moscow, Russia
*
Author to whom correspondence should be addressed.
Received: 9 December 2020 / Revised: 16 February 2021 / Accepted: 17 February 2021 / Published: 20 February 2021
(This article belongs to the Special Issue Animal Venoms and Their Components: Molecular Mechanisms of Action)
Cobra venoms contain three-finger toxins (TFT) including α-neurotoxins efficiently binding nicotinic acetylcholine receptors (nAChRs). As shown recently, several TFTs block GABAA receptors (GABAARs) with different efficacy, an important role of the TFTs central loop in binding to these receptors being demonstrated. We supposed that the positive charge (Arg36) in this loop of α-cobratoxin may explain its high affinity to GABAAR and here studied α-neurotoxins from African cobra N. melanoleuca venom for their ability to interact with GABAARs and nAChRs. Three α-neurotoxins, close homologues of the known N. melanoleuca long neurotoxins 1 and 2, were isolated and sequenced. Their analysis on Torpedocalifornica and α7 nAChRs, as well as on acetylcholine binding proteins and on several subtypes of GABAARs, showed that all toxins interacted with the GABAAR much weaker than with the nAChR: one neurotoxin was almost as active as α-cobratoxin, while others manifested lower activity. The earlier hypothesis about the essential role of Arg36 as the determinant of high affinity to GABAAR was not confirmed, but the results obtained suggest that the toxin loop III may contribute to the efficient interaction of some long-chain neurotoxins with GABAAR. One of isolated toxins manifested different affinity to two binding sites on Torpedo nAChR. View Full-Text
Keywords: binding sites; cobra venom; GABAA receptor; neurotoxin; three-finger toxin; nicotinic acetylcholine receptor; acetylcholine binding protein binding sites; cobra venom; GABAA receptor; neurotoxin; three-finger toxin; nicotinic acetylcholine receptor; acetylcholine binding protein
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MDPI and ACS Style

Son, L.; Kryukova, E.; Ziganshin, R.; Andreeva, T.; Kudryavtsev, D.; Kasheverov, I.; Tsetlin, V.; Utkin, Y. Novel Three-Finger Neurotoxins from Naja melanoleuca Cobra Venom Interact with GABAA and Nicotinic Acetylcholine Receptors. Toxins 2021, 13, 164. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13020164

AMA Style

Son L, Kryukova E, Ziganshin R, Andreeva T, Kudryavtsev D, Kasheverov I, Tsetlin V, Utkin Y. Novel Three-Finger Neurotoxins from Naja melanoleuca Cobra Venom Interact with GABAA and Nicotinic Acetylcholine Receptors. Toxins. 2021; 13(2):164. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13020164

Chicago/Turabian Style

Son, Lina; Kryukova, Elena; Ziganshin, Rustam; Andreeva, Tatyana; Kudryavtsev, Denis; Kasheverov, Igor; Tsetlin, Victor; Utkin, Yuri. 2021. "Novel Three-Finger Neurotoxins from Naja melanoleuca Cobra Venom Interact with GABAA and Nicotinic Acetylcholine Receptors" Toxins 13, no. 2: 164. https://0-doi-org.brum.beds.ac.uk/10.3390/toxins13020164

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