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DYRK1A Inhibitors and Perspectives for the Treatment of Alzheimer's Disease.
de Souza, Márcia Maria; Cenci, Arthur Ribeiro; Teixeira, Kerolain Faoro; Machado, Valkiria; Mendes Schuler, Majory Christina Garcia; Gonçalves, Ana Elisa; Paula Dalmagro, Ana; André Cazarin, Camila; Gomes Ferreira, Leonardo Luiz; de Oliveira, Aldo Sena; Andricopulo, Adriano Defini.
Afiliação
  • de Souza MM; School of Health Sciences, Graduate Program in Pharmaceutical Sciences, UNIVALI, Rua Uruguai, 458 F6 lab 206 Campus I, Centro, Itajai, SC, 88302-202, Brazil.
  • Cenci AR; Department of Exact Sciences and Education, Federal University of Santa Catarina, R. João Pessoa, 2750 - Velha, 89036-002, Blumenau, SC, Brazil.
  • Teixeira KF; Department of Exact Sciences and Education, Federal University of Santa Catarina, R. João Pessoa, 2750 - Velha, 89036-002, Blumenau, SC, Brazil.
  • Machado V; Department of Exact Sciences and Education, Federal University of Santa Catarina, R. João Pessoa, 2750 - Velha, 89036-002, Blumenau, SC, Brazil.
  • Mendes Schuler MCG; Department of Exact Sciences and Education, Federal University of Santa Catarina, R. João Pessoa, 2750 - Velha, 89036-002, Blumenau, SC, Brazil.
  • Gonçalves AE; School of Health Sciences, Graduate Program in Pharmaceutical Sciences, UNIVALI, Rua Uruguai, 458 F6 lab 206 Campus I, Centro, Itajai, SC, 88302-202, Brazil.
  • Paula Dalmagro A; School of Health Sciences, Graduate Program in Pharmaceutical Sciences, UNIVALI, Rua Uruguai, 458 F6 lab 206 Campus I, Centro, Itajai, SC, 88302-202, Brazil.
  • André Cazarin C; School of Health Sciences, Graduate Program in Pharmaceutical Sciences, UNIVALI, Rua Uruguai, 458 F6 lab 206 Campus I, Centro, Itajai, SC, 88302-202, Brazil.
  • Gomes Ferreira LL; Laboratory of Medicinal and Computational Chemistry, Center for Research and Innovation in Biodiversity and Drug Discovery, Institute of Physics of São Carlos, University of São Paulo, São Carlos-SP, Brazil.
  • de Oliveira AS; Laboratory of Medicinal and Computational Chemistry, Center for Research and Innovation in Biodiversity and Drug Discovery, Institute of Physics of São Carlos, University of São Paulo, São Carlos-SP, Brazil.
  • Andricopulo AD; Laboratory of Medicinal and Computational Chemistry, Center for Research and Innovation in Biodiversity and Drug Discovery, Institute of Physics of São Carlos, University of São Paulo, São Carlos-SP, Brazil.
Curr Med Chem ; 30(6): 669-688, 2023.
Article em En | MEDLINE | ID: mdl-35726411
BACKGROUND: Alzheimer's disease (AD) is a chronic neurodegenerative disease and the most common form of dementia, especially in the elderly. Due to the increase in life expectancy, in recent years, there has been an excessive growth in the number of people affected by this disease, causing serious problems for health systems. In recent years, research has been intensified to find new therapeutic approaches that prevent the progression of the disease. In this sense, recent studies indicate that the dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) gene, which is located on chromosome 21q22.2 and overexpressed in Down syndrome (DS), may play a significant role in developmental brain disorders and early onset neurodegeneration, neuronal loss and dementia in DS and AD. Inhibiting DYRK1A may serve to stop the phenotypic effects of its overexpression and, therefore, is a potential treatment strategy for the prevention of ageassociated neurodegeneration, including Alzheimer-type pathology. OBJECTIVE: In this review, we investigate the contribution of DYRK1A inhibitors as potential anti-AD agents. METHODS: A search in the literature to compile an in vitro dataset including IC50 values involving DYRK1A was performed from 2014 to the present day. In addition, we carried out structure-activity relationship studies based on in vitro and in silico data. RESULTS: molecular modeling and enzyme kinetics studies indicate that DYRK1A may contribute to AD pathology through its proteolytic process, reducing its kinase specificity. CONCLUSION: further evaluation of DYRK1A inhibitors may contribute to new therapeutic approaches for AD.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteínas Quinases / Doença de Alzheimer Limite: Aged / Humans Idioma: En Revista: Curr Med Chem Assunto da revista: QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Brasil País de publicação: Emirados Árabes Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Proteínas Quinases / Doença de Alzheimer Limite: Aged / Humans Idioma: En Revista: Curr Med Chem Assunto da revista: QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Brasil País de publicação: Emirados Árabes Unidos