Chemo-proteomics in antimalarial target identification and engagement

Bailey, BL; Nguyen, W; Cowman, AF; Sleebs, BE

Author(s): Bailey, BL; Nguyen, W; Cowman, AF; Sleebs, BE;
Details: Publication Year 2023-05-26,Volume 43,Issue #6,Page 2303-2351
Journal Title: Medicinal Research Reviews
Abstract: Humans have lived in tenuous battle with malaria over millennia. Today, while much of the world is free of the disease, areas of South America, Asia, and Africa still wage this war with substantial impacts on their social and economic development. The threat of widespread resistance to all currently available antimalarial therapies continues to raise concern. Therefore, it is imperative that novel antimalarial chemotypes be developed to populate the pipeline going forward. Phenotypic screening has been responsible for the majority of the new chemotypes emerging in the past few decades. However, this can result in limited information on the molecular target of these compounds which may serve as an unknown variable complicating their progression into clinical development. Target identification and validation is a process that incorporates techniques from a range of different disciplines. Chemical biology and more specifically chemo-proteomics have been heavily utilized for this purpose. This review provides an in-depth summary of the application of chemo-proteomics in antimalarial development. Here we focus particularly on the methodology, practicalities, merits, and limitations of designing these experiments. Together this provides learnings on the future use of chemo-proteomics in antimalarial development.
Publisher: Wiley
Keywords: antimalarial; chemical probe; malaria; target engagement; target identification
Research Division(s): Chemical Biology; Infectious Diseases And Immune Defence
PubMed ID: 37232495
Publisher's Version: https://doi.org/10.1002/med.21975
Open Access at Publisher's Site: https://doi.org/10.1002/med.21975
Terms of Use/Rights Notice: Refer to copyright notice on published article.

Creation Date: 2023-11-20 03:24:04

Last Modified: 2023-11-20 03:25:02