Epigenetic Inhibitors as Alzheimer's Disease Therapeutic Agents.
Chem Pharm Bull (Tokyo)
; 72(7): 630-637, 2024.
Article
en En
| MEDLINE
| ID: mdl-38945939
ABSTRACT
Alzheimer's disease (AD) is the leading cause of senile dementia, and the rapid increase in the frequency of AD cases has been attributed to population aging. However, current drugs have difficulty adequately suppressing symptoms and there is still a medical need for symptomatic agents. On the other hand, it has recently become clear that epigenetic dysfunctions are deeply involved in the development of cognitive impairments. Therefore, epigenetics-related proteins have attracted much attention as drug targets for AD. Early-developed epigenetic inhibitors were inappropriate for AD treatment because of their limited potential for oral administration, blood-brain barrier penetration, high target selectivity, and sufficient dose-limiting toxicity which are essential properties for small molecule drugs targeting chronic neurodegenerative diseases such as AD. In recent years, drug discovery studies have been actively performed to overcome such problems and several novel inhibitors targeting the epigenetics-related proteins are of interest as promising AD therapeutic agents. Here, we review the small molecule inhibitors of histone deacetylase (HDAC), lysine-specific demethylase 1 (LSD1) or bromodomains and extra-terminal domain (BET) protein, that enable memory function improvement in AD model mice.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Epigénesis Genética
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Histona Demetilasas
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Inhibidores de Histona Desacetilasas
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Enfermedad de Alzheimer
Límite:
Animals
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Humans
Idioma:
En
Revista:
Chem Pharm Bull (Tokyo)
/
Chem. pharm. bull
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Chemical & pharmaceutical bulletin
Año:
2024
Tipo del documento:
Article