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Last Updated: 26/09/2023
Towards a cure for Malaria: Computational Design and Synthes
Objectives
To develop an early lead inhibitor against the malaria protein kinase PfCLK3.
Specific Objectives:
- Conduct hit to lead on TCMDC-135051. Previous studies discovered a potent and selective inhibitor to PfCLK3, namely TCMDC-135051. The plan is to further develop this inhibitor in a hit to lead programme.
- Screen for novel chemical matter and develop in a hit to lead campaign. A high throughput assay for PfCLK3 has been developed that will be used to screen new compounds. Hits will be optimised in a hit to lead programme
- Test front running molecules for properties that meet MMV criteria for subsequent Lead to Candidate optimisation.
Principal Institution
Principal Investigators / Focal Persons
Rationale and Abstract
This protein kinase plays an essential role in RNA splicing and has been validated by us to be a target with the potential to offer prophylactic, curative and transmission blocking activity. To deliver on this aim compounds will be synthesised and assessed in vitro and in vivo assay platforms what will allow to test the properties of optimised PfCLK3 inhibitors against MMV’s Target Candidate Profiles (TCPs) for compounds for Lead to Candidate development.
External reference
Thematic Categories
Date
Sep 2021 — Mar 2025
Funding Details
Engineering and Physical Sciences Research Council (EPSRC), United Kingdom
Grant number : 2607115
Project Site
Related Resources
