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Small molecules targeting γ-secretase and their potential biological applications
The γ-secretase is a large transmembrane protein complex composed of four distinct units. It has aroused numerous attention over the past two decades as its intriguing role in mediating intramembrane proteolysis. γ-Secretase controls the cleavage of a broad ranged substrates, part of which have impl...
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Published in: | European journal of medicinal chemistry 2022-03, Vol.232, p.114169-114169, Article 114169 |
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Main Authors: | , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | The γ-secretase is a large transmembrane protein complex composed of four distinct units. It has aroused numerous attention over the past two decades as its intriguing role in mediating intramembrane proteolysis. γ-Secretase controls the cleavage of a broad ranged substrates, part of which have implicated in the pathogenesis of Alzheimer's disease, inflammation, and tumorigenesis. The disclosure of the atomic structure of the γ-secretase complex through cryo-EM in recent years has facilitated the understanding of its physiological roles, as well as enabled rational design of novel γ-secretase targeting molecules. This review highlights the recent progress of γ-secretase inhibitors and modulators under either clinical or preclinical stages, as well as their potential uses against various biological indications.
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•Summary of structure and functions of γ-secretase complex.•Conclusive review of γ-secretase targeting small molecules under clinical trials.•Advances of γ-secretase modulators and their potential anti-AD activity.•Advances of γ-secretase inhibitors and their potential biological activity. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2022.114169 |