Paired associative stimulation (PAS) and Alzheimer’s disease (AD)

Tampi, Rajesh R.

doi:10.1017/s1041610222000813

Cited by 7 publications

(2 citation statements)

References 16 publications

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“…The primary hallmark of Alzheimer’s disease is the accumulation of β-amyloid proteins in the synapses of the cortical neurons and the formation of tau tangles inside the neurons due to the twisting of tau protein fibers. These accumulations lead to the neurons’ death by hampering the transfer of signals among the neurons [ 7 , 8 ]. The accumulation of β-amyloid proteins between the synaptic spaces results from the action of the BACE-1 (β-site amyloid precursor protein cleaving enzyme 1) enzyme.…”

Section: Introductionmentioning

confidence: 99%

Scaffold Morphing and In Silico Design of Potential BACE-1 (β-Secretase) Inhibitors: A Hope for a Newer Dawn in Anti-Alzheimer Therapeutics

et al. 2023

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Alzheimer’s disease (AD) is the prime cause of 65–80% of dementia cases and is caused by plaque and tangle deposition in the brain neurons leading to brain cell degeneration. β-secretase (BACE-1) is a key enzyme responsible for depositing extracellular plaques made of β-amyloid protein. Therefore, efforts are being applied to develop novel BACE-1 enzyme inhibitors to halt plaque build-up. In our study, we analyzed some Elenbecestat analogues (a BACE-1 inhibitor currently in clinical trials) using a structure-based drug design and scaffold morphing approach to achieve a superior therapeutic profile, followed by in silico studies, including molecular docking and pharmacokinetics methodologies. Among all the designed compounds, SB306 and SB12 showed good interactions with the catalytic dyad motifs (Asp228 and Asp32) of the BACE-1 enzyme with drug-likeliness properties and a high degree of thermodynamic stability confirmed by the molecular dynamic and stability of the simulated system indicating the inhibitory nature of the SB306 and SB12 on BACE 1.

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Section: Introductionmentioning

confidence: 99%

Scaffold Morphing and In Silico Design of Potential BACE-1 (β-Secretase) Inhibitors: A Hope for a Newer Dawn in Anti-Alzheimer Therapeutics

et al. 2023

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“…While no significant differences between the active and control rPAS groups on DLPFC plasticity or working memory performance emerged, post hoc analyses suggested several potential promising lines of further inquiry. Advantages of using TMS in older populations include minimal adverse effects, no harmful effects on cognition, and the absence of any drug interactions, and its success in treating cognitive and behavioral aspects of dementia make continued explorations of the methodology, as in the paper by Kumar et al (2023), warranted (Tampi, 2023).…”

mentioning

confidence: 99%