Yeast-based high-throughput screens for discovery of kinase inhibitors for neglected diseases

Autor(es)

Tavella, T. A. ; Cassiano, G. C. ; Maranhao Costa, Fabio Trindade ; Sunnerhagen, P. ; Bilsland, E. ; Donev, R

• Tipo de documento: Artigo Científico
• Fonte: ADVANCES IN PROTEIN CHEMISTRY AND STRUCTURAL BIOLOGY, VOL 124: PROTEIN KINASES IN DRUG DISCOVERY; v. 124, p. 35-pg., 2021-01-01.

Resumo

The discovery and development of a new drug is a complex, time consuming and costly process that typically takes over 10 years and costs around 1 billion dollars from bench to market. This scenario makes the discovery of novel drugs targeting neglected tropical diseases (NTDs), which afflict in particular people in low-income countries, prohibitive. Despite the intensive use of High-Throughput Screening (HTS) in the past decades, the speed with which new drugs come to the market has remained constant, generating doubts about the efficacy of this approach. Here we review a few of the yeast-based high-throughput approaches that can work synergistically with parasite-based, in vitro, or in silico methods to identify and optimize novel antiparasitic compounds. These yeast-based methods range from HTP screens to identify novel hits against promising parasite kinase targets to the identification of potential antiparasitic kinase inhibitors extracted from databases of yeast chemical genetic screens. (AU)

• Processo FAPESP: 19/27626-3 - Identificação de novos tratamentos antimaláricos através de uma abordagem de "reposicionamento de fármacos" centrada no alvo
• Beneficiário: Tatyana Almeida Tavella
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 15/20774-6 - Identificação de inibidores de quinases com atividade antimalárica baseado em análises de quimiogenômica, bioinformática e fenotípicas: enfoque em Plasmodium vivax.
• Beneficiário: Gustavo Capatti Cassiano
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 12/16525-2 - Plasmodium vivax: patogênese e infectividade
• Beneficiário: Fabio Trindade Maranhão Costa
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• Processo FAPESP: 15/03553-6 - Engenharia genética de leveduras para a descoberta de novos medicamentos
• Beneficiário: Elizabeth Bilsland
• Modalidade de apoio: Auxílio à Pesquisa - Jovens Pesquisadores