Projects per year
The protozoan parasite Trypanosoma brucei is the causative agent of African sleeping sickness, and there is an urgent unmet need for improved treatments. Parasite protein kinases are attractive drug targets, provided that the host and parasite kinomes are sufficiently divergent to allow specific inhibition to be achieved. Current drug discovery efforts are hampered by the fact that comprehensive assay panels for parasite targets have not yet been developed. Here, we employ a kinase-focused chemoproteomics strategy that enables the simultaneous profiling of kinase inhibitor potencies against more than SO endogenously expressed T. brucei kinases in parasite cell extracts. The data reveal that T. brucei kinases are sensitive to typical kinase inhibitors with nanomolar potency and demonstrate the potential for the development of species-specific inhibitors.
|Number of pages||8|
|Journal||ACS Chemical Biology|
|Early online date||21 Aug 2012|
|Publication status||Published - 2012|
- DRUG TARGET
- AFRICAN SLEEPING SICKNESS
- EUKARYOTIC PROTEIN-KINASES
FingerprintDive into the research topics of 'Chemical Proteomic Analysis Reveals the Drugability of the Kinome of Trypanosoma brucei'. Together they form a unique fingerprint.
- 2 Finished
Aref#d: 20731. The Biosynthesis of Glycoproteins in Trypanosoma Brucei: Basic and Translational Research
1/10/08 → 31/05/14
Aref#d: 19815. Wellcome Trust Centre for Drug Discovery (Strategic Award)
Fairlamb, A., Ferguson, M. & Frearson, J.
1/01/08 → 31/12/12