Thermal proteome profiling for interrogating protein interactions

A Mateus, N Kurzawa, I Becher, S Sridharan… - Molecular systems …, 2020 - embopress.org
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 …

Recent advances in identifying protein targets in drug discovery

J Ha, H Park, J Park, SB Park - Cell chemical biology, 2021 - cell.com
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 …

Recent advances in isobaric labeling and applications in quantitative proteomics

MK Sivanich, TJ Gu, DN Tabang, L Li - Proteomics, 2022 - Wiley Online Library
Mass spectrometry (MS) has emerged at the forefront of quantitative proteomic techniques.
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 …

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 …

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 …

[HTML][HTML] Plasmodium falciparum resistance to ACTs: Emergence, mechanisms, and outlook

FA Siddiqui, X Liang, L Cui - … Journal for Parasitology: Drugs and Drug …, 2021 - Elsevier
Emergence and spread of resistance in Plasmodium falciparum to the frontline treatment
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 …

Photoaffinity labelling strategies for mapping the small molecule–protein interactome

NR Burton, P Kim, KM Backus - Organic & biomolecular chemistry, 2021 - pubs.rsc.org
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 …

Drug target identification in tissues by thermal proteome profiling

A Mateus, N Kurzawa, J Perrin… - Annual Review of …, 2022 - annualreviews.org
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 …