Novel anti-senile dementia lead compound

Abstract

The invention discloses a novel anti-senile dementia lead compound, which is characterized in that: an amino acid sequence of the lead compound is amino terminal-VTLWWG-carboxyl terminal. A peptide sequence is designed on the basis of a quantitative structural function relation model of a peptide, is detected through an atomic force microscope scanning technology, and is further obtained with cytotoxicity experimental evaluation. The lead compound has a good inhibiting effect on the aggregation of a toxic body-Abeta which leads to senile dementia, and can be further developed into a senile dementia resisting medicament.

Description

technical field [0001] The invention relates to a novel anti-senile dementia lead compound, in particular to an anti-senile dementia toxicant Aβ lead compound. Background technique [0002] At present, there are at least 35 million people in the world suffering from Alzheimer's disease, and the annual death rate is rising. The total annual global cost is estimated to reach 200 billion U.S. dollars. Studies have shown that Aβ (Amyloid β-peptide) oligomers are significant toxic substances in patients with Alzheimer's disease, so inhibiting the generation of Aβ oligomers is the most effective way to prevent the occurrence of Alzheimer's disease. effective strategy. However, there is currently no effective method for the design of Aβ inhibitors, mainly facing three serious challenges: 1. Lack of effective high-throughput screening methods: experimental screening methods need to synthesize and purify Aβ, which is undoubtedly a challenge for the screening of a large number of com...

AI Technical Summary

Problems solved by technology

However, there is currently no effective method for the design of Aβ inhibitors, mainly facing three serious challenges: 1. Lack of effective high-throughput screening methods: experimental screening methods need to synthesize and purify Aβ, which is undoubtedly a challenge for the screening of a large number of compounds Time-consuming, expensive and impractical

2. Lack of high-resolution structures of Aβ oligomers: Aβ oligomers are in a metastable state, so it is difficult to obtain their structures using X-ray diffraction and NMR techniques, making rational drug design based on structures difficult to achieve

3. Lack of understanding of the mechanism of Aβ self-assembly: including which part of the peptide plays a key role in the process of amyloid fibril generation; what are the pathways and intermediates related to seed and fiber generation; whether Aβ has affinity to specific receptors body; how Aβ generates the toxic body and what is the mechanism of toxicity

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