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- Title
Driving antimalarial design through understanding of target mechanism.
- Authors
Calic, Petar P. S.; Mansouri, Mahta; Scammells, Peter J.; McGowan, Sheena
- Abstract
Malaria continues to be a global health threat, affecting approximately 219 million people in 2018 alone. The recurrent development of resistance to existing antimalarials means that the design of new drug candidates must be carefully considered. Understanding of drug target mechanism can dramatically accelerate early-stage target-based development of novel antimalarials and allows for structural modifications even during late-stage preclinical development. Here, we have provided an overview of three promising antimalarial molecular targets, PfDHFR, PfDHODH and PfA-M1, and their associated inhibitors which demonstrate how mechanism can inform drug design and be effectively utilised to generate compounds with potent inhibitory activity.
- Subjects
DRUG design; MALARIA; ANTIMALARIALS; WORLD health; TARGETED drug delivery
- Publication
Biochemical Society Transactions, 2020, Vol 48, Issue 5, p2067
- ISSN
0300-5127
- Publication type
Article
- DOI
10.1042/BST20200224