期刊
CHEMMEDCHEM
卷 17, 期 14, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202200174
关键词
Drug Discovery; Fluorescent probes; Malaria; Mass spectrometry; Proteomics
资金
- European Union's Horizon 2020 research and innovation programme under the Marie Skodowska-Curie grant [101022421]
- Marie Curie Actions (MSCA) [101022421] Funding Source: Marie Curie Actions (MSCA)
Activity-based protein profiling (ABPP) is a widely used method in malaria research that utilizes small molecular probes to study enzymatic activity, achieving significant advancements in the study of Plasmodium proteases, metabolic pathways, and target identification for antimalarials.
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.
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