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

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

  • Autores: Tatyana Almeida Tavella, Gustavo Capatti Cassiano, Fabio Trindade Maranhão Costa, Per Sunnerhagen, Elizabeth Bilsland
  • Ano de Publicação: 2021
  • Journal: Advances in Protein Chemistry and Structural Biology, vol 124, pp 275-309
  • Link: https://doi.org/10.1016/bs.apcsb.2020.09.007

CHAPTER 8 OF THE BOOK «PROTEIN KINASES IN DRUG DISCOVERY»

 

ABSTRACT

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.

 

KEYWORDS

Yeast; High-throughput; Neglected diseases; Kinase inhibitors; Drug discovery; Drug screening.

Chapter 7

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About GHTM

GHTM is a R&D Center that brings together researchers from IHMT with a track record in Tropical Medicine and International/Global Health. It aims at strengthening Portugal's role as a leading partner in the development and implementation of a global health research agenda. Our evidence-based interventions contribute to the promotion of equity in health and to improve the health of populations.

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