Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors
Chagas disease, a parasitic disease caused by Trypanosoma cruzi, is a major public health burden in poor rural populations of Central and South America and a serious emerging threat outside the endemic region, since the number of infections in non-endemic countries continues to rise. In order to dev...
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todo:paper_10736085_v_n_p1_Mild2023-10-03T16:02:55Z Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors Mild, J.G. Fernandez, L.R. Gayet, O. Iovanna, J. Dusetti, N. Edreira, M.M. BRET Drug screening Protein–protein interactions Trypanosoma cruzi Bioluminescence Developing countries Diagnosis Energy transfer Enzyme activity Health risks Phosphorescence Bioluminescence resonance energy transfer BRET Drug screening Functional characteristics Protein interaction Screening compounds Suitable conditions Trypanosoma cruzi Drug interactions antitrypanosomal agent protein binding protozoal protein Central America chemistry drug effect fluorescence resonance energy transfer HEK293 cell line human metabolism molecular library pharmacology preclinical study procedures protein analysis South America Trypanosoma cruzi Central America Drug Evaluation, Preclinical Fluorescence Resonance Energy Transfer HEK293 Cells Humans Protein Binding Protein Interaction Maps Protozoan Proteins Small Molecule Libraries South America Trypanocidal Agents Trypanosoma cruzi Chagas disease, a parasitic disease caused by Trypanosoma cruzi, is a major public health burden in poor rural populations of Central and South America and a serious emerging threat outside the endemic region, since the number of infections in non-endemic countries continues to rise. In order to develop more efficient anti-trypanosomal treatments to replace the outdated therapies, new molecular targets need to be explored and new drugs discovered. Trypanosoma cruzi has distinctive structural and functional characteristics with respect to the human host. These exclusive features could emerge as interesting drug targets. In this work, essential and differential protein–protein interactions for the parasite, including the ribosomal P proteins and proteins involved in mRNA processing, were evaluated in a bioluminescence resonance energy transfer-based assay as a starting point for drug screening. Suitable conditions to consider using this simple and robust methodology to screening compounds and natural extracts able to inhibit protein–protein interactions were set in living cells and lysates. © 2018 Springer Science+Business Media, LLC, part of Springer Nature INPR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_10736085_v_n_p1_Mild |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
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R-134 |
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Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
BRET Drug screening Protein–protein interactions Trypanosoma cruzi Bioluminescence Developing countries Diagnosis Energy transfer Enzyme activity Health risks Phosphorescence Bioluminescence resonance energy transfer BRET Drug screening Functional characteristics Protein interaction Screening compounds Suitable conditions Trypanosoma cruzi Drug interactions antitrypanosomal agent protein binding protozoal protein Central America chemistry drug effect fluorescence resonance energy transfer HEK293 cell line human metabolism molecular library pharmacology preclinical study procedures protein analysis South America Trypanosoma cruzi Central America Drug Evaluation, Preclinical Fluorescence Resonance Energy Transfer HEK293 Cells Humans Protein Binding Protein Interaction Maps Protozoan Proteins Small Molecule Libraries South America Trypanocidal Agents Trypanosoma cruzi |
| spellingShingle |
BRET Drug screening Protein–protein interactions Trypanosoma cruzi Bioluminescence Developing countries Diagnosis Energy transfer Enzyme activity Health risks Phosphorescence Bioluminescence resonance energy transfer BRET Drug screening Functional characteristics Protein interaction Screening compounds Suitable conditions Trypanosoma cruzi Drug interactions antitrypanosomal agent protein binding protozoal protein Central America chemistry drug effect fluorescence resonance energy transfer HEK293 cell line human metabolism molecular library pharmacology preclinical study procedures protein analysis South America Trypanosoma cruzi Central America Drug Evaluation, Preclinical Fluorescence Resonance Energy Transfer HEK293 Cells Humans Protein Binding Protein Interaction Maps Protozoan Proteins Small Molecule Libraries South America Trypanocidal Agents Trypanosoma cruzi Mild, J.G. Fernandez, L.R. Gayet, O. Iovanna, J. Dusetti, N. Edreira, M.M. Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| topic_facet |
BRET Drug screening Protein–protein interactions Trypanosoma cruzi Bioluminescence Developing countries Diagnosis Energy transfer Enzyme activity Health risks Phosphorescence Bioluminescence resonance energy transfer BRET Drug screening Functional characteristics Protein interaction Screening compounds Suitable conditions Trypanosoma cruzi Drug interactions antitrypanosomal agent protein binding protozoal protein Central America chemistry drug effect fluorescence resonance energy transfer HEK293 cell line human metabolism molecular library pharmacology preclinical study procedures protein analysis South America Trypanosoma cruzi Central America Drug Evaluation, Preclinical Fluorescence Resonance Energy Transfer HEK293 Cells Humans Protein Binding Protein Interaction Maps Protozoan Proteins Small Molecule Libraries South America Trypanocidal Agents Trypanosoma cruzi |
| description |
Chagas disease, a parasitic disease caused by Trypanosoma cruzi, is a major public health burden in poor rural populations of Central and South America and a serious emerging threat outside the endemic region, since the number of infections in non-endemic countries continues to rise. In order to develop more efficient anti-trypanosomal treatments to replace the outdated therapies, new molecular targets need to be explored and new drugs discovered. Trypanosoma cruzi has distinctive structural and functional characteristics with respect to the human host. These exclusive features could emerge as interesting drug targets. In this work, essential and differential protein–protein interactions for the parasite, including the ribosomal P proteins and proteins involved in mRNA processing, were evaluated in a bioluminescence resonance energy transfer-based assay as a starting point for drug screening. Suitable conditions to consider using this simple and robust methodology to screening compounds and natural extracts able to inhibit protein–protein interactions were set in living cells and lysates. © 2018 Springer Science+Business Media, LLC, part of Springer Nature |
| format |
INPR |
| author |
Mild, J.G. Fernandez, L.R. Gayet, O. Iovanna, J. Dusetti, N. Edreira, M.M. |
| author_facet |
Mild, J.G. Fernandez, L.R. Gayet, O. Iovanna, J. Dusetti, N. Edreira, M.M. |
| author_sort |
Mild, J.G. |
| title |
Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| title_short |
Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| title_full |
Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| title_fullStr |
Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| title_full_unstemmed |
Optimization of a Bioluminescence Resonance Energy Transfer-Based Assay for Screening of Trypanosoma cruzi Protein/Protein Interaction Inhibitors |
| title_sort |
optimization of a bioluminescence resonance energy transfer-based assay for screening of trypanosoma cruzi protein/protein interaction inhibitors |
| url |
http://hdl.handle.net/20.500.12110/paper_10736085_v_n_p1_Mild |
| work_keys_str_mv |
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1807317506522611712 |