Venom Peptide Toxins Targeting the Outer Pore Region of Transient Receptor Potential Vanilloid 1 in Pain: Implications for Analgesic Drug Development.

Venom Peptide Toxins Targeting the Outer Pore Region of Transient Receptor Potential Vanilloid 1 in Pain: Implications for Analgesic Drug Development.
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DOI:
10.3390/ijms23105772
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发表时间:
2022-05-21
影响因子:
5.6
通讯作者:
--
中科院分区:
生物学2区
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--
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瞬时受体电位香草酸1(TRPV1)离子通道在外周伤害性感受通路中起重要作用。TRPV1是一种多模式受体,可被多种类型的配体和疼痛刺激物(如有害热和质子)激活,并导致各种急性和慢性疼痛状况。因此,TRPV1正在成为治疗各种疼痛病症的新的治疗靶点。值得注意的是,从有毒动物中分离出的各种肽通过与TRPV1的外孔区域结合而有效地和选择性地控制TRPV1的激活和抑制。本文将重点介绍毒液衍生肽与TRPV1的这一部分相互作用以控制受体功能的机制,以及这些机制如何推动新型镇痛药的开发。
The transient receptor potential vanilloid 1 (TRPV1) ion channel plays an important role in the peripheral nociceptive pathway. TRPV1 is a polymodal receptor that can be activated by multiple types of ligands and painful stimuli, such as noxious heat and protons, and contributes to various acute and chronic pain conditions. Therefore, TRPV1 is emerging as a novel therapeutic target for the treatment of various pain conditions. Notably, various peptides isolated from venomous animals potently and selectively control the activation and inhibition of TRPV1 by binding to its outer pore region. This review will focus on the mechanisms by which venom-derived peptides interact with this portion of TRPV1 to control receptor functions and how these mechanisms can drive the development of new types of analgesics.
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