Tau as a therapeutic target for Alzheimer's disease.
Tau as a therapeutic target for Alzheimer's disease.
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Tau是阿尔茨海默氏病的治疗靶标。
DOI：
10.2174/156720511796717195
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发表时间：
2011-09
影响因子：
2.1
通讯作者：
Krishnamurthy PK
中科院分区：
文献类型：
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作者：
Boutajangout A;Sigurdsson EM;Krishnamurthy PK
神经原纤维缠结（nft）是阿尔茨海默病（AD）的病理标志之一，主要由微管相关蛋白tau的过度磷酸化形式的聚集体组成。很可能是激酶和磷酸酶活性的不平衡导致tau蛋白的异常磷酸化和随后的聚集。正在开发的广泛的治疗方法包括抑制tau激酶，增强磷酸酶活性，促进微管稳定性，减少tau聚集体的形成和/或通过小分子药物或免疫治疗手段增强其清除。大多数这些有希望的方法仍处于临床前开发阶段，而有些方法已进入II期临床试验。通过这些研究，可能会获得一种可行的治疗阿尔茨海默病和相关病变的方法。
Neurofibrillary tangles (NFTs) are one of the pathological hallmarks of Alzheimer’s disease (AD) and are primarily composed of aggregates of hyperphosphorylated forms of the microtubule associated protein tau. It is likely that an imbalance of kinase and phosphatase activities leads to the abnormal phosphorylation of tau and subsequent aggregation. The wide ranging therapeutic approaches that are being developed include to inhibit tau kinases, to enhance phosphatase activity, to promote microtubule stability, and to reduce tau aggregate formation and/or enhance their clearance with small molecule drugs or by immunotherapeutic means. Most of these promising approaches are still in preclinical development whilst some have progressed to Phase II clinical trials. By pursuing these lines of study, a viable therapy for AD and related tauopathies may be obtained.