Department of Experimental Medicine, University of Genoa, Genoa, Italy.
IRCCS Ospedale Policlinico San Martino, Genoa, Italy.
Biofactors. 2023 May-Jun;49(3):502-511. doi: 10.1002/biof.1930. Epub 2023 Jan 23.
Tau is a macrotubule-associated protein primarily involved in the stabilization of the cytoskeleton. Under normal conditions, phosphorylation reduces the affinity of tau for tubulin, allowing the protein to detach from microtubules and ensuring the system dynamics in neuronal cells. However, hyperphosphorylated tau aggregates into paired helical filaments, the main constituents of neurofibrillary tangles found in the brains of patients with Alzheimer's disease and other tauopathies. In this review, we provide an overview of the structure of tau and the pathophysiological roles of tau phosphorylation. We also evaluate the major protein kinases involved and discuss the progress made in the development of drug therapies aimed at inhibiting tau kinases.
tau 是一种微管相关蛋白,主要参与细胞骨架的稳定。在正常情况下,磷酸化降低了 tau 与微管的亲和力,使蛋白质从微管上脱离,从而确保神经元细胞中的系统动力学。然而,过度磷酸化的 tau 聚集形成成对螺旋丝,这是阿尔茨海默病和其他 tau 病患者大脑中神经原纤维缠结的主要成分。在这篇综述中,我们概述了 tau 的结构和 tau 磷酸化的病理生理作用。我们还评估了涉及的主要蛋白激酶,并讨论了在开发旨在抑制 tau 激酶的药物治疗方面取得的进展。