Department of Pharmacy (DIFAR), University of Genoa, 16132 Genoa, Italy.
Department of Experimental Medicine (DIMES), University of Genoa, 16132 Genoa, Italy.
Int J Mol Sci. 2022 Jun 25;23(13):7061. doi: 10.3390/ijms23137061.
We propose a model to explain the pathogenesis of Alzheimer's disease (AD) based on the theory that any disease affecting a healthy organism originates from a bistable feedback loop that shifts the system from a physiological to a pathological condition. We focused on the known double inhibitory loop involving the cellular prion protein (PrPC) and the enzyme BACE1 that produces amyloid-beta (Aβ) peptides. BACE1 is inhibited by PrPC, but its inhibitory activity is lost when PrPC binds to Aβ oligomers (Aβo). Excessive Aβo formation would switch the loop to a pathogenic condition involving the Aβo-PrPC-mGluR5 complex, Fyn kinase activation, tau, and NMDAR phosphorylation, ultimately leading to neurodegeneration. Based on the emerging role of cyclic nucleotides in Aβ production, and thereby in synaptic plasticity and cognitive processes, cAMP and cGMP can be considered as modulatory factors capable of inducing the transition from a physiological steady state to a pathogenic one. This would imply that critical pharmacological targets for AD treatment lie within pathways that lead to an imbalance of cyclic nucleotides in neurons. If this hypothesis is confirmed, it will provide precise indications for the development of preventive or therapeutic treatments for the disease.
我们提出了一个基于以下理论的阿尔茨海默病(AD)发病机制模型:任何影响健康生物体的疾病都源于双稳态反馈回路,该回路将系统从生理状态转变为病理状态。我们专注于已知的涉及细胞朊病毒蛋白(PrPC)和产生淀粉样β肽(Aβ)的酶 BACE1 的双抑制环。BACE1 被 PrPC 抑制,但当 PrPC 与 Aβ寡聚物(Aβo)结合时,其抑制活性丧失。过量的 Aβo 形成会使环路转变为涉及 Aβo-PrPC-mGluR5 复合物、Fyn 激酶激活、tau 和 NMDAR 磷酸化的致病状态,最终导致神经退行性变。基于环核苷酸在 Aβ产生中的新兴作用,以及在突触可塑性和认知过程中的作用,cAMP 和 cGMP 可以被认为是能够诱导从生理稳态到致病状态转变的调节因子。这意味着 AD 治疗的关键药理学靶点位于导致神经元中环核苷酸失衡的途径内。如果这一假设得到证实,它将为该疾病的预防或治疗提供精确的治疗靶点。