Watson Judy J, Allen Shelley J, Dawbarn David
University of Bristol, Bristol, UK.
BioDrugs. 2008;22(6):349-59. doi: 10.2165/0063030-200822060-00002.
Chronic pain presents a huge economic and social burden, with existing treatments largely unable to satisfy medical needs. Recently, studies have shown that nerve growth factor (NGF) is a major mediator of inflammatory and neuropathic pain, providing a new therapeutic target. Although originally discovered as a trophic factor for sympathetic and sensory neurons during development, it now appears that in adults, levels of NGF are elevated in many acute and chronic pain conditions. Furthermore, preclinical animal models of inflammatory and neuropathic pain also show increased NGF levels, while the sequestration of NGF alleviates the associated hyperalgesia. The molecular mechanisms involved are being elucidated. This review briefly examines pain signaling pathways and describes currently available analgesics. It then investigates the approaches taken in targeting NGF-mediated pain. Current options being explored include the development of humanized monoclonal antibodies to NGF or its tyrosine kinase receptor TrkA (also known as neurotrophic tyrosine kinase receptor, type 1 [NTRK1]), and the sequestration of NGF using TrkA domain 5 (TrkAd5), a soluble receptor protein that binds NGF with picomolar affinity. Administration of either antibodies or TrkAd5 has been shown to be effective in a number of preclinical models of pain, including cystitis, osteoarthritis, UV irradiation (sunburn), and skeletal bone pain due to fracture or cancer. Other possible future therapies examined in this review include small-molecule TrkA antagonists, which target either the extracellular NGF binding domain of TrkA or its intracellular tyrosine kinase domain.
慢性疼痛带来了巨大的经济和社会负担,现有的治疗方法在很大程度上无法满足医疗需求。最近的研究表明,神经生长因子(NGF)是炎症性和神经性疼痛的主要介质,这提供了一个新的治疗靶点。尽管NGF最初是在发育过程中作为交感神经和感觉神经元的营养因子被发现的,但现在看来,在成年人中,NGF水平在许多急性和慢性疼痛情况下都会升高。此外,炎症性和神经性疼痛的临床前动物模型也显示NGF水平升高,而抑制NGF可减轻相关的痛觉过敏。其中涉及的分子机制正在被阐明。本综述简要研究了疼痛信号通路并描述了目前可用的镇痛药。然后研究了针对NGF介导的疼痛所采取的方法。目前正在探索的选择包括开发针对NGF或其酪氨酸激酶受体TrkA(也称为神经营养酪氨酸激酶受体1型[NTRK1])的人源化单克隆抗体,以及使用TrkA结构域5(TrkAd5)来抑制NGF,TrkAd5是一种可溶性受体蛋白,能以皮摩尔亲和力结合NGF。在多种疼痛的临床前模型中,包括膀胱炎、骨关节炎、紫外线照射(晒伤)以及骨折或癌症引起的骨骼疼痛,已证明给予抗体或TrkAd5均有效。本综述中研究的其他可能的未来疗法包括小分子TrkA拮抗剂,其靶向TrkA的细胞外NGF结合结构域或其细胞内酪氨酸激酶结构域。
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