Thermal proteome profiling for interrogating protein interactions
Thermal proteome profiling (TPP) is based on the principle that, when subjected to heat,
proteins denature and become insoluble. Proteins can change their thermal stability upon …
proteins denature and become insoluble. Proteins can change their thermal stability upon …
Recent advances in identifying protein targets in drug discovery
Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …
Recent advances in isobaric labeling and applications in quantitative proteomics
Mass spectrometry (MS) has emerged at the forefront of quantitative proteomic techniques.
Liquid chromatography‐mass spectrometry (LC‐MS) can be used to determine abundances …
Liquid chromatography‐mass spectrometry (LC‐MS) can be used to determine abundances …
Sources of antifungal drugs
G Vanreppelen, J Wuyts, P Van Dijck, P Vandecruys - Journal of Fungi, 2023 - mdpi.com
Due to their eukaryotic heritage, the differences between a fungal pathogen's molecular
makeup and its human host are small. Therefore, the discovery and subsequent …
makeup and its human host are small. Therefore, the discovery and subsequent …
CETSA and thermal proteome profiling strategies for target identification and drug discovery of natural products
Y Tu, L Tan, H Tao, Y Li, H Liu - Phytomedicine, 2023 - Elsevier
Background Monitoring target engagement at various stages of drug development is
essential for natural product (NP)-based drug discovery and development. The cellular …
essential for natural product (NP)-based drug discovery and development. The cellular …
Dual plasmepsin-targeting antimalarial agents disrupt multiple stages of the malaria parasite life cycle
P Favuzza, M de Lera Ruiz, JK Thompson, T Triglia… - Cell host & …, 2020 - cell.com
Artemisin combination therapy (ACT) is the main treatment option for malaria, which is
caused by the intracellular parasite Plasmodium. However, increased resistance to ACT …
caused by the intracellular parasite Plasmodium. However, increased resistance to ACT …
[HTML][HTML] Plasmodium falciparum resistance to ACTs: Emergence, mechanisms, and outlook
Emergence and spread of resistance in Plasmodium falciparum to the frontline treatment
artemisinin-based combination therapies (ACTs) in the epicenter of multidrug resistance of …
artemisinin-based combination therapies (ACTs) in the epicenter of multidrug resistance of …
The artemisinin-induced dormant stages of Plasmodium falciparum exhibit hallmarks of cellular quiescence/senescence and drug resilience
J Tripathi, M Stoklasa, S Nayak, K En Low… - Nature …, 2024 - nature.com
Recrudescent infections with the human malaria parasite, Plasmodium falciparum,
presented traditionally the major setback of artemisinin-based monotherapies. Although the …
presented traditionally the major setback of artemisinin-based monotherapies. Although the …
Photoaffinity labelling strategies for mapping the small molecule–protein interactome
Nearly all FDA approved drugs and bioactive small molecules exert their effects by binding
to and modulating proteins. Consequently, understanding how small molecules interact with …
to and modulating proteins. Consequently, understanding how small molecules interact with …
Drug target identification in tissues by thermal proteome profiling
Drug target deconvolution can accelerate the drug discovery process by identifying a drug's
targets (facilitating medicinal chemistry efforts) and off-targets (anticipating toxicity effects or …
targets (facilitating medicinal chemistry efforts) and off-targets (anticipating toxicity effects or …