Konar Mouli, Ghosh Debasis, Samanta Sourav, Govindaraju Thimmaiah
Bioorganic Chemistry Laboratory, New Chemistry Unit and School of Advanced Materials (SAMat), Jawaharlal Nehru Centre for Advanced Scientific Research Jakkur P.O. Bengaluru 560064 Karnataka India
RSC Chem Biol. 2021 Dec 23;3(2):220-226. doi: 10.1039/d1cb00235j. eCollection 2022 Feb 9.
Amyloid beta (Aβ) aggregation species-associated cellular stress instigates cytotoxicity and adverse cellular stiffness in neuronal cells. The study and modulation of these adverse effects demand immediate attention to tackle Alzheimer's disease (AD). We present a design, synthesis and evaluation of Aβ14-23 peptidomimetics with cyclic dipeptide (CDP) units at defined positions. Our study identified Akd with CDP units at the middle, N- and C-termini as a potent candidate to understand and ameliorate Aβ aggregation-induced cellular toxicity and adverse stiffness.
淀粉样β蛋白(Aβ)聚集相关的细胞应激会引发神经元细胞的细胞毒性和不良的细胞硬度。对这些不良反应的研究和调节需要立即引起关注,以应对阿尔茨海默病(AD)。我们展示了一种在特定位置带有环二肽(CDP)单元的Aβ14 - 23拟肽的设计、合成和评估。我们的研究确定,在中间、N端和C端带有CDP单元的Akd是理解和改善Aβ聚集诱导的细胞毒性和不良硬度的有力候选物。