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A Lysosome-Targeting hNEU1 Inhibitor Treats Myocardial Infarction: A Potential Therapeutic Breakthrough
Wen Zhou1,2, Wanxiang Yang1, Ping Jiang1
1Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
Journal of Medicinal Chemistry
|September 10, 2024
Summary
A novel lysosome-targeting compound, OsMo, effectively inhibits human NEU1 (hNEU1) linked to myocardial infarction. OsMo shows promise for treating heart damage by improving autophagy regulation and demonstrating efficacy in vivo.
Area of Science:
- Biochemistry
- Pharmacology
- Cardiovascular Medicine
Background:
- N-acetylneuraminidase 1 (NEU1) overexpression is linked to myocardial infarction.
- Developing effective human NEU1 (hNEU1) inhibitors is challenging, with viral NEU1 (viNEU1) inhibitors showing limited hNEU1 efficacy.
Purpose of the Study:
- To design and evaluate novel lysosome-targeting compounds for hNEU1 inhibition.
- To investigate the therapeutic potential of these compounds in myocardial infarction models.
Main Methods:
- Design of lysosome-targeting compounds derived from oseltamivir.
- Evaluation of compound activity, lysosomal accumulation, and pharmacophore release.
- Assessment of autophagy regulation and efficacy in myocardial infarction models in vivo.
Main Results:
- OsMo, a novel compound, demonstrated potent hNEU1 inhibition by accumulating pharmacophores within lysosomes.
- OsMo effectively regulated abnormal autophagy during myocardial injury.
- OsMo showed superior efficacy in treating myocardial infarction in vivo with acceptable pharmacokinetics.
Conclusions:
- Lysosome-targeting drug design is a promising strategy for myocardial injuries associated with hNEU1.
- OsMo represents a potential therapeutic agent for myocardial infarction due to its targeted inhibition and efficacy.
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