| Author | Moreira, Bernardo Pereira | |
| Author | Armstrong, Tom | |
| Author | Batista, Izabella Cristina Andrade | |
| Author | Tavares, Naiara Clemente | |
| Author | Pires, Camilla Valente | |
| Author | Mourão, Marina de Moraes | |
| Author | Falcone, Franco H. | |
| Author | Dekker, Lodewijk V. | |
| Access date | 2020-05-19T19:26:59Z | |
| Available date | 2020-05-19T19:26:59Z | |
| Document date | 2020 | |
| Citation | 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. | pt_BR |
| ISSN | 2470-1343 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/41310 | |
| Language | eng | pt_BR |
| Publisher | American Chemical Society | pt_BR |
| Rights | restricted access | pt_BR |
| Title | BODIPY-Labeled ATP Analogues in the Development and Validation of a Fluorescence Polarization-Based Assay for Screening of Kinase Inhibitors | pt_BR |
| Type | Article | |
| DOI | 10.1021/acsomega.9b03344 | |
| Abstract | 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. | pt_BR |
| Affilliation | 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. | pt_BR |
| Affilliation | University of Nottingham. School of Chemistry. Nottingham NG7 2RD, United Kingdom. | pt_BR |
| Affilliation | 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. | pt_BR |
| Affilliation | 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. | pt_BR |
| Affilliation | 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. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | 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. | pt_BR |
| Affilliation | University of Nottingham. School of Pharmacy. Division of Biomolecular Science and Medicinal Chemistry. Nottingham NG7 2RD, United Kingdom. | pt_BR |
| Subject | Protein kinases | pt_BR |
| Subject | BODIPY-Labeled ATP | pt_BR |
| Embargo date | 2035-01-01 | |
