Griffin Jeddidiah W D, Bradshaw Patrick C
Department of Natural Sciences, Mars Hill University, Mars Hill, NC, 28754, USA.
Department of Biomedical Sciences, Quillen College of Medicine, East Tennessee State University, Johnson City, TN, 37614, USA.
Protein J. 2021 Apr;40(2):175-183. doi: 10.1007/s10930-021-09965-w. Epub 2021 Feb 10.
Alzheimer's disease (AD) patients could benefit from a more effective treatment than the current FDA-approved options. Because amyloid-beta (Aβ) is thought to play a central role in AD pathogenesis, many experimental drugs attempt to reduce Aβ-induced pathology. Preventing amyloid accumulation may be a more effective strategy than clearing Aβ plaques after they form. If preventing Aβ accumulation can treat or prevent AD, then understanding Aβ primary nucleation may aid rational drug design. This study examines Aβ residue interaction networks and reports network and structural observations that may provide insight into primary nucleation. While many studies identify structural features of Aβ that promote aggregation, this study reports features that may resist primary nucleation by examining Aβ42 studies in more and less polar solvents. In Aβ42 in a less polar solvent (PDB ID: 1IYT), Val24 and Ile31 have higher betweenness and residue centrality values. This may be due to a predicted interaction between Val24 and Ile31. Residues in the central hydrophobic cluster (CHC) of Aβ40 and Aβ42 had significantly higher betweenness values compared to the average betweenness of the structures, highlighting the CHC's reported role in oligomerization. The predicted interaction between Val24 and Ile31 may reduce the likelihood of primary nucleation of Aβ.
与目前美国食品药品监督管理局(FDA)批准的治疗方案相比,阿尔茨海默病(AD)患者可能会从更有效的治疗中受益。由于β淀粉样蛋白(Aβ)被认为在AD发病机制中起核心作用,许多实验性药物试图减少Aβ诱导的病理变化。防止淀粉样蛋白积累可能比在其形成后清除Aβ斑块是一种更有效的策略。如果防止Aβ积累可以治疗或预防AD,那么了解Aβ的初级成核可能有助于合理的药物设计。本研究考察了Aβ残基相互作用网络,并报告了可能有助于深入了解初级成核的网络和结构观察结果。虽然许多研究确定了促进Aβ聚集的结构特征,但本研究通过考察在极性较高和较低的溶剂中的Aβ42研究,报告了可能抵抗初级成核的特征。在极性较低的溶剂中的Aβ42(蛋白质数据银行ID:1IYT)中,Val24和Ile31具有较高的介数和残基中心性值。这可能是由于预测的Val24和Ile31之间的相互作用。与结构的平均介数相比,Aβ40和Aβ 的中心疏水簇(CHC)中的残基具有显著更高的介数,突出了CHC在寡聚化中所报道的作用。预测的Val24和Ile31之间的相互作用可能会降低Aβ初级成核的可能性。