Department of Neurology, Danish Headache Center, Copenhagen University Hospital - Rigshospitalet, Copenhagen, Denmark.
Department of Neurology, Danish Headache Center, Copenhagen University Hospital - Rigshospitalet, Copenhagen, Denmark.
Neurobiol Dis. 2023 Jan;176:105946. doi: 10.1016/j.nbd.2022.105946. Epub 2022 Dec 5.
Migraine is a widespread and debilitating neurological condition affecting more than a billion people worldwide. Thus, more effective migraine therapies are highly needed. In the last decade, two endogenous neuropeptides, calcitonin gene-related peptide (CGRP) and pituitary adenylate cyclase-activating peptide (PACAP), were identified to be implicated in migraine. Recently, introduction of monoclonal antibodies (mAbs) blocking the CGRP is the most important advance in migraine therapy for decades. However, 40% of patients are unresponsive to these new drugs. We believe that PACAP may be involved in these patients. Like CGRP, PACAP is located to sensory nerve fibers, it dilates cranial arteries, it causes migraine when infused into patients and it is a peptide that lends itself to antibody therapy. Also, recent studies suggest that the PACAP pathway is independent of the CGRP pathway. Understanding the signaling pathways of PACAP may therefore lead to identification of novel therapeutic targets of particular interest in patients unresponsive to anti-CGRP therapy. Accordingly, neutralizing mAb to PACAP is currently in clinical phase II development. The aim of the present review is, therefore, to give a thorough account of the existing data on PACAP, its receptors and its relation to migraine.
偏头痛是一种广泛存在且使人虚弱的神经系统疾病,影响着全球超过 10 亿人。因此,我们急需更有效的偏头痛治疗方法。在过去的十年中,两种内源性神经肽,降钙素基因相关肽(CGRP)和垂体腺苷酸环化酶激活肽(PACAP),被认为与偏头痛有关。最近,阻断 CGRP 的单克隆抗体(mAbs)的引入是偏头痛治疗几十年来最重要的进展。然而,仍有 40%的患者对这些新药没有反应。我们认为 PACAP 可能与这些患者有关。与 CGRP 一样,PACAP 位于感觉神经纤维中,它扩张颅动脉,当注入患者体内时会引起偏头痛,并且它是一种适合抗体治疗的肽。此外,最近的研究表明,PACAP 途径独立于 CGRP 途径。因此,了解 PACAP 的信号通路可能会导致发现对 CGRP 治疗无反应的患者特别感兴趣的新型治疗靶点。因此,中和 PACAP 的 mAb 目前正在进行临床二期开发。因此,本综述的目的是全面阐述 PACAP、其受体及其与偏头痛的关系的现有数据。
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