The Impact of Activity-Based Protein Profiling in Malaria Drug Discovery.
Publication Date
2022-05-04Journal Title
ChemMedChem
ISSN
1860-7179
Publisher
Wiley
Language
en
Type
Article
This Version
AO
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Carvalho, L. A., & Lopes Bernardes, G. (2022). The Impact of Activity-Based Protein Profiling in Malaria Drug Discovery.. ChemMedChem https://doi.org/10.1002/cmdc.202200174
Abstract
Activity-based protein profiling (ABPP) is an approach used at the interface of chemical biology and proteomics that uses small molecular probes to provide dynamic fingerprints of enzymatic activity in complex proteomes. Malaria is a disease caused by Plasmodium parasites with a significant death burden and for which new therapies are actively being sought. Here, we compile the main achievements from ABPP studies in malaria and highlight the probes used and the different downstream platforms for data analysis. ABPP has excelled at studying Plasmodium cysteine proteases and serine hydrolase families, the targeting of the proteasome and metabolic pathways, and in the deconvolution of targets and mechanisms of known antimalarials. Despite the major impact in the field, many antimalarials and enzymatic families in Plasmodium remain to be studied, which suggests ABPP will be an evergreen technique in the field.
Keywords
Review, Reviews, Drug Discovery, Fluorescent probes, Malaria, Mass spectrometry, Proteomics
Sponsorship
European Commission Horizon 2020 (H2020) Marie Sk?odowska-Curie actions (101022421)
Identifiers
cmdc202200174
External DOI: https://doi.org/10.1002/cmdc.202200174
This record's URL: https://www.repository.cam.ac.uk/handle/1810/337303
Rights
Licence:
http://creativecommons.org/licenses/by/4.0/
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