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ProteomicsThermal proteome profiling of MMV897615
The target deconvolution of MMV897615 was evaluated using thermal proteome profiling (TPP), a chemical proteomics approach based on the stabilisation of protein targets upon ligand binding. In these TPP experiments we used a whole-cell strategy, exposing cells rather than lysates to the drug
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2023-03-09 | PXD034937 | Pride
Acyl-coa synthetases Drug target Thermal proteome profiling Plasmodium falciparum 
ProteomicsDiscovery, target identification and lead optimisation of a quinazoline series with potent anti-Chagasic activity
We next used an approach to determine the direct binding of quinazolines to their target(s). A protein can be stabilised or destabilised through the binding of a ligand, altering that proteins thermostability. Such alterations in thermostability can cause a ligated protein to denature at a different...
ORGANISM(S): Trypanosoma cruzi Dm28c 
2025-04-22 | PXD050235 | Pride
Drug target Trypanosoma cruzi Thermal proteome profiling 
ProteomicsDrug target deconvolution in Plasmodium falciparum using thermal proteomics profiling
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 prot...
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2022-10-13 | PXD025182 | Pride
Lysine trna synthetase Thermal proteome profiling Plasmodium falciparum 
ProteomicsTarget deconvolution in Plasmodium falciparum using pulldowns
Parasite lysates were centrifuged (20,000 g, 4°C, 15 min). Beads (blank and with linker attached) were washed 3× with water then twice with lysis buffer. The lysate (~2 mg total protein) was first incubated with 2 mg blank beads for 30 min at 4°C with rotating agitation. The lysate was divided into ...
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2022-10-15 | PXD033740 | Pride
Pulldown Plasmodium falciparum Drug target Chemical proteomics 
ProteomicsSterol 14-alpha demethylase (CYP51) activity in Leishmania donovani is likely dependent upon cytochrome P450 reductase 1
Liposomal amphotericin B is an important frontline drug for the treatment of visceral leishmaniasis, a neglected disease of poverty. The mechanism of action of amphotericin B (AmB) is thought to involve interaction with ergosterol and other ergostane sterols, resulting in disruption of the integrity...
ORGANISM(S): Leishmania donovani BPK282A1 
2024-06-21 | PXD052472 | Pride
Visceral leishmaniasis Mechanism of action P450 reductase and sterol 14-alpha demethylase (cyp51) Drug resistance Leishmania Sterol metabolism 
ProteomicsUbiquitination in treated T. cruzi parasites
T. cruzi epimastigotes in the logarithmic growth phase (3×106 cells mL-1) were incubated for 12h with bortezomib (1.8 µM), GNF6702 (2.9 µM) or compound 1 (24 µM), equivalent to 8× the EC50 values of each compound. Controls were incubated in the presence of diluent (DMSO). Cells were harvested by cen...
ORGANISM(S): Trypanosoma cruzi Dm28c 
2022-02-17 | PXD027524 | Pride
Ubiquitination Trypanosoma cruzi Proteasome 
ProteomicsMultiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial
Samples were reduced by the addition of TCEP (25 mM final concentration) and incubated at 37 ºC for 10 min. Alkylation was carried out by the addition of iodoacetamide (25 mM final concentration) and incubated at RT for 1 h in the dark. Samples were then digested by the addition of 1:50 LysC (Wako, ...
ORGANISM(S): Leishmania donovani BPK282A1 
2021-07-18 | PXD023780 | Pride
Thermal proteome profiling Leishmania Oxidosqualene synthase 
ProteomicsThermal proteome profiling in Cryptosporidium parvum
Cryptosporidium lacks tools that can identify the targets of emerging compounds that have been developed against this parasite. Thermal proteomic profiling is an unbiased approach that fulfils this unmet need by detecting changes in the thermal stability of target proteins upon the binding of their ...
ORGANISM(S): Cryptosporidium parvum Iowa II 
2023-06-13 | PXD037942 | Pride
Drug target Lysyl-trna synthetase Cryptosporodium parvum Thermal proteome profiling 
ProteomicsMMV2224 project isothermal TPP experiments
Isothermal TPP was performed essentially as previously described (Milne, R., et al., Toolkit of Approaches To Support Target-Focused Drug Discovery for Plasmodium falciparum Lysyl tRNA Synthetase. ACS Infect Dis, 2022. 8(9): p. 1962–1974). In this instance P. falciparum lysates incubated ± drug were...
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2026-09-07 | PXD075163 | Pride
Isothermal proteome profiling Mmv22224 Plasmodium falciparum 
ProteomicsMMV2224 project pulldown experimental data
Chemical pulldown - sample processing, fractionation, protein identification and quantitation All aspects of sample processing, TMT labelling, fractionation by HPLC and LC–MS/MS, and protein identification and quantitation were described previously (Milne, R., et al., Toolkit of Approaches To Suppo...
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2026-09-07 | PXD075229 | Pride
Pulldown Kinase inhibitors Plasmodium falciparum 
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