Up-Regulation of Akt and Nav1.8 in BmK I-Induced Pain

Zhou, Guokun; Jiao, Yun-Lu; Zhou, You; Qin, Shichao; Tao, Jie; Jiang, Feng; Tan, Zhiyuan; Ji, Yonghua

doi:10.1007/s12264-018-0222-x

Cited by 5 publications

(4 citation statements)

References 8 publications

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“…Among them, neurotoxins possessing nociceptive effects like BmK I, a major peptide isolated from the Chinese Buthus martensii venom that is non-lethal for mammals, have been shown to induce spontaneous pain and hyperalgesia upon subcutaneous injections in rat hind paw [ 115 , 116 ]. Its activity involves the TTX-S Nav1.6 and TTX-R Nav1.8 channels which are over-expressed when BmK I is administered to rodents [ 117 ]. BmK I potentiates Nav1.6 and Nav1.8 currents revealing an important role for these channels in the modulation of spontaneous pain and mechanical allodynia [ 118 - 120 ].…”

Section: Scorpion Toxins Interacting With Pain-related Ion Channelsmentioning

confidence: 99%

Pain-related toxins in scorpion and spider venoms: a face to face with ion channels

Diochot

2021

J. Venom. Anim. Toxins incl. Trop. Dis

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Pain is a common symptom induced during envenomation by spiders and scorpions. Toxins isolated from their venom have become essential tools for studying the functioning and physiopathological role of ion channels, as they modulate their activity. In particular, toxins that induce pain relief effects can serve as a molecular basis for the development of future analgesics in humans. This review provides a summary of the different scorpion and spider toxins that directly interact with pain-related ion channels, with inhibitory or stimulatory effects. Some of these toxins were shown to affect pain modalities in different animal models providing information on the role played by these channels in the pain process. The close interaction of certain gating-modifier toxins with membrane phospholipids close to ion channels is examined along with molecular approaches to improve selectivity, affinity or bioavailability in vivo for therapeutic purposes.

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Section: Scorpion Toxins Interacting With Pain-related Ion Channelsmentioning

confidence: 99%

Pain-related toxins in scorpion and spider venoms: a face to face with ion channels

Diochot

2021

J. Venom. Anim. Toxins incl. Trop. Dis

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“…The long-chain scorpion toxins composed of 58-76 amino acid residues mainly act on voltage-gated sodium channels (VGSCs), while the short-chain scorpion toxins containing 28-40 amino acid residues generally target K + or Cl − channels [9] (Figure 1B). Based on their physiological effects on VGSC gating and binding properties, the long-chain toxins can be further classified into two categories: α-toxins, such as BmK I, a 64-residue α-like toxin isolated from BmK [2], and BmK αIV, a novel cloned 68-residue polypeptide, binding to neurotoxin receptor site 3 of the VGSC, with inhibitory effects on the fast inactivation of VGSCs (Figure 2). β-toxins, which bind to receptor site 4 such as BmK IT2 as well as BmK AEP, two 64-residue inhibitory β-toxins [10], and BmK AS, a 66-residue β-like toxin, could shift the threshold of VGSCs activation to more negative membrane potentials [11][12][13][14] (Figure 2).…”

Section: Structures Of Scorpion Toxin Peptides (A)mentioning

confidence: 99%

“…Pain seriously damages human health and quality of life, so it is of importance to find effective analgesic targets and drugs. Nav channels (VGSCs) are transmembrane proteins responsible for generation and conduction of APs (action potentials) in excitable cells [1][2][3]. Of the nine functional α subunits (Nav1.1-1.9), Nav1.1, Nav1.3, Nav1.6, Nav1.7, Nav1.8, and Nav1.9 are distributed in primary sensory neurons, playing a crucial role in nociception and chronic pain [4].…”

Section: Analgesic Effects Of Bmk Toxins Against Vgscsmentioning

confidence: 99%

“…Recent advances underlying medical studies have illuminated that several neurological disorders such as epilepsy, chronic pain, multiple sclerosis, stroke, brain tumor etc. are induced by dysfunction of membrane ion channels [1][2][3]. Up to now, multiple drugs specifically targeting ion channels have been designed to treat the diseases [4].…”

Section: Introductionmentioning

confidence: 99%

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Scorpion Toxins from Buthus martensii Karsch (BmK) as Potential Therapeutic Agents for Neurological Disorders: State of the Art and Beyond

Wang¹,

Zhang²,

Zhu³

et al. 2021

Medical Toxicology

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Scorpions are fascinating creatures which became residents of the planet well before human beings dwelled on Earth. Scorpions are always considered as a figure of fear, causing notable pain or mortality throughout the world. Their venoms are cocktails of bioactive molecules, called toxins, which are responsible for their toxicity. Fortunately, medical researchers have turned the life-threatening toxins into life-saving therapeutics. From Song Dynasty in ancient China, scorpions and their venoms have been applied in traditional medicine for treating neurological disorders, such as pain, stroke, and epilepsy. Neurotoxins purified from Chinese scorpion Buthus Martensii Karsch (BmK) are considered as the main active ingredients, which act on membrane ion channels. Long-chain toxins of BmK, composed of 58-76 amino acids, could specifically recognize voltage-gated sodium channels (VGSCs). Short-chain BmK toxins, containing 28-40 amino acids, are found to modulate the potassium or chloride channels. These components draw attention as useful scaffolds for drug-design in order to tackle the emerging global medical threats. In this chapter, we aim to summarize the most promising candidates that have been isolated from BmK venoms for drug development.

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Dezocine relieves the postoperative hyperalgesia in rats through suppressing the hyper-action of Akt1/GSK-3β pathway

Gong

Xu²,

Liu³

et al. 2022

Exp Brain Res

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Up-Regulation of Akt and Nav1.8 in BmK I-Induced Pain

Cited by 5 publications

References 8 publications

Pain-related toxins in scorpion and spider venoms: a face to face with ion channels

Pain-related toxins in scorpion and spider venoms: a face to face with ion channels

Scorpion Toxins from Buthus martensii Karsch (BmK) as Potential Therapeutic Agents for Neurological Disorders: State of the Art and Beyond

Dezocine relieves the postoperative hyperalgesia in rats through suppressing the hyper-action of Akt1/GSK-3β pathway

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