Towards a cure for Malaria: Computational Design and Synthes
Lead Research Organisation:
University of Glasgow
Department Name: School of Chemistry
Abstract
"This project aims to develop an Early Lead inhibitor against the malaria protein kinase PfCLK3. 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 we will synthesise and assess compounds in vitro and in vivo assay platforms what will allow the student to test the properties of optimised PfCLK3 inhibitors against MMV's Target Candidate Profiles (TCPs) for compounds for Lead to Candidate development.
The project objectives:
1. Conduct hit to lead on TCMDC-135051.
Our previous studies discovered a potent and selective inhibitor to PfCLK3, namely TCMDC-135051. We plan to further develop this inhibitor in a hit to lead programme.
2. Screen for novel chemical matter and develop in a hit to lead campaign. We have developed a high throughput assay for PfCLK3 that will be used to screen new compounds. Hits will be optimised in a hit to lead programme
3. Test front running molecules for properties that meet MMV criteria for subsequent Lead to Candidate optimisation. "
To deliver on this aim we will synthesise and assess compounds in vitro and in vivo assay platforms what will allow the student to test the properties of optimised PfCLK3 inhibitors against MMV's Target Candidate Profiles (TCPs) for compounds for Lead to Candidate development.
The project objectives:
1. Conduct hit to lead on TCMDC-135051.
Our previous studies discovered a potent and selective inhibitor to PfCLK3, namely TCMDC-135051. We plan to further develop this inhibitor in a hit to lead programme.
2. Screen for novel chemical matter and develop in a hit to lead campaign. We have developed a high throughput assay for PfCLK3 that will be used to screen new compounds. Hits will be optimised in a hit to lead programme
3. Test front running molecules for properties that meet MMV criteria for subsequent Lead to Candidate optimisation. "
Organisations
People |
ORCID iD |
| Andrew Jamieson (Primary Supervisor) | |
| Skye Brettell (Student) |
Studentship Projects
| Project Reference | Relationship | Related To | Start | End | Student Name |
|---|---|---|---|---|---|
| EP/T517896/1 | 30/09/2020 | 29/09/2025 | |||
| 2607115 | Studentship | EP/T517896/1 | 30/09/2021 | 30/03/2025 | Skye Brettell |