Proteomics

Dataset Information

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Drug target deconvolution in Plasmodium falciparum using thermal proteomics profiling

ABSTRACT: Early identification of a compound’s mode of action can greatly benefit the discovery process. Thermal proteomics profiling (TPP) is a powerful, unbiased tool that can be used to identify potential ligands of protein targets. TPP takes advantage of the fact that a ligand binding to its target protein can significantly stabilise that protein, increasing its melting temperature (Tm). We previously optimised this technique for use in drug target deconvolution in the kinetoplastid parasite, Leishmania donovani1 and here report the optimisation and validation of TPP in the malaria-causing parasite P. falciparum.

INSTRUMENT(S):

ORGANISM(S): Plasmodium Falciparum (isolate 3d7)

TISSUE(S): Cell Culture

DISEASE(S): Plasmodium Falciparum Malaria

SUBMITTER: Victoriano Corpas-Lopez  

LAB HEAD: Dr. Susan Wyllie

PROVIDER: PXD025182 | Pride | 2022-10-13

REPOSITORIES: Pride

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Publications

There is a pressing need for new medicines to prevent and treat malaria. Most antimalarial drug discovery is reliant upon phenotypic screening. However, with the development of improved target validation strategies, target-focused approaches are now being utilized. Here, we describe the development of a toolkit to support the therapeutic exploitation of a promising target, lysyl tRNA synthetase (<i>Pf</i>KRS). The toolkit includes resistant mutants to probe resistance mechanisms and on-target en  ...[more]

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