Receptor Pharmacology Unit, National Institute on Aging, Baltimore, MD 21224, USA.
Curr Alzheimer Res. 2012 Jan;9(1):110-9. doi: 10.2174/156720512799015055.
The extensive prevalence of Alzheimer's disease (AD) places a tremendous burden physiologically, socially and economically upon those directly suffering and those caring for sufferers themselves. Considering the steady increases in numbers of patients diagnosed with Alzheimer's, the number of effective pharmacotherapeutic strategies to tackle the disease is still relatively few. As with many other neurodegenerative mechanisms, AD, is characterized by the continued presence and accumulation of cytotoxic protein aggregates, i.e. of beta-amyloid and the microtubule associated protein, tau. Therefore, one novel therapeutic avenue for the treatment of AD may be the actual targeting of factors that control protein synthesis, packaging and degradation. One of the prime cellular targets that, if effectively modulated, could accomplish this is the endoplasmic reticulum (ER). The ER can not only control cellular protein synthesis, trafficking and degradation but it is also closely associated with cytoprotective mechanisms, including calcium ion regulation and unfolded protein responses. This review will delineate some of the most important functional physiological features of the ER that, if effectively modulated, could result in beneficial amelioration or remediation of the negative cellular aspects of AD initiation and progression. While not a classical drug target, even with minimal levels of beneficial modulation, its multifactorial efficacy may amplify small effects resulting in significant therapeutic efficacy.
阿尔茨海默病(AD)的广泛流行给直接患病者及其护理者在生理、社会和经济方面带来了巨大的负担。考虑到被诊断患有阿尔茨海默病的患者人数不断增加,用于治疗该疾病的有效药物治疗策略仍然相对较少。与许多其他神经退行性机制一样,AD 的特征是持续存在和积累细胞毒性蛋白聚集物,即β-淀粉样蛋白和微管相关蛋白 tau。因此,治疗 AD 的一种新的治疗途径可能是实际针对控制蛋白质合成、包装和降解的因素。如果能有效调节,一个主要的细胞靶标就是内质网(ER)。内质网不仅可以控制细胞的蛋白质合成、运输和降解,而且还与细胞保护机制密切相关,包括钙离子调节和未折叠蛋白反应。这篇综述将阐述内质网的一些最重要的功能生理特征,如果能有效地调节这些特征,可能会对 AD 发病和进展的负面细胞方面产生有益的改善或补救作用。虽然内质网不是一个经典的药物靶点,但即使是最小程度的有益调节,其多效性也可能会放大小的作用,从而产生显著的治疗效果。