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2035-01-01
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BODIPY-LABELED ATP ANALOGUES IN THE DEVELOPMENT AND VALIDATION OF A FLUORESCENCE POLARIZATION-BASED ASSAY FOR SCREENING OF KINASE INHIBITORS
Moreira, Bernardo Pereira et al. | Data do documento: 2020
Autor(es)
Moreira, Bernardo Pereira
Armstrong, Tom
Batista, Izabella Cristina Andrade
Tavares, Naiara Clemente
Pires, Camilla Valente
Mourão, Marina de Moraes
Falcone, Franco H.
Dekker, Lodewijk V.
Afiliação
Biomedizinisches Forschungszentrum Seltersberg, Institut für Parasitologie, Justus-Liebig-Universität Gießen, 35392 Gießen, Germany / Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil / University of Nottingham. School of Pharmacy. Division of Molecular Therapeutics and Formulation. Nottingham NG7 2RD, United Kingdom.
University of Nottingham. School of Chemistry. Nottingham NG7 2RD, United Kingdom.
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil / University of Nottingham. School of Pharmacy. Division of Molecular Therapeutics and Formulation. Nottingham NG7 2RD, United Kingdom.
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil / University of Nottingham. School of Pharmacy. Division of Molecular Therapeutics and Formulation. Nottingham NG7 2RD, United Kingdom.
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil / University of Nottingham. School of Pharmacy. Division of Molecular Therapeutics and Formulation. Nottingham NG7 2RD, United Kingdom.
Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil.
Biomedizinisches Forschungszentrum Seltersberg, Institut für Parasitologie, Justus-Liebig-Universität Gießen, 35392 Gießen, Germany / University of Nottingham. School of Pharmacy. Division of Molecular Therapeutics and Formulation. Nottingham NG7 2RD, United Kingdom.
University of Nottingham. School of Pharmacy. Division of Biomolecular Science and Medicinal Chemistry. Nottingham NG7 2RD, United Kingdom.
Resumo em Inglês
The screening of compound libraries to identify small-molecule modulators of specific biological targets is crucial in the process for the discovery of novel therapeutics and molecular probes. Considering the need for simple single-tool assay technologies with which one could monitor “all” kinases, we developed a fluorescence polarization (FP)-based assay to monitor the binding capabilities of protein kinases to ATP. We used BODIPY ATP-y-S as a probe to measure the shift in the polarization of a light beam when passed through the sample. We were able to optimize the assay using commercial Protein Kinase A (PKA) and H7 efficiently inhibited the binding of the probe when added to the reaction. Furthermore, we were able to employ the assay in a high-throughput fashion and validate the screening of a set of small molecules predicted to dock into the ATP-binding site of PKA. This will be useful to screen larger libraries of compounds that may target protein kinases by blocking ATP binding.
Palavras-chave em inglês
Protein kinases
BODIPY-Labeled ATP
 
Editor
American Chemical Society
Referência
MOREIRA, Bernardo Pereira et al. BODIPY-Labeled ATP Analogues in the Development and Validation of a Fluorescence Polarization-Based Assay for Screening of Kinase Inhibitors. ACS Omega, v. 5, n. 16, p. 9064−9070, 2020.
DOI
10.1021/acsomega.9b03344
ISSN
2470-1343