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 …

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 …

Proteome integral solubility alteration: a high-throughput proteomics assay for target deconvolution

M Gaetani, P Sabatier, AA Saei… - Journal of proteome …, 2019 - ACS Publications
Various agents, including drugs as well as nonmolecular stimuli, induce alterations in the
physicochemical properties of proteins in cell lysates, living cells, and organisms. These …

Nonparametric analysis of thermal proteome profiles reveals novel drug-binding proteins

D Childs, K Bach, H Franken, S Anders… - Molecular & Cellular …, 2019 - ASBMB
Detecting the targets of drugs and other molecules in intact cellular contexts is a major
objective in drug discovery and in biology more broadly. Thermal proteome profiling (TPP) …

Comparison of quantitative mass spectrometric methods for drug target identification by thermal proteome profiling

AL George, FR Sidgwick, JE Watt… - Journal of Proteome …, 2023 - ACS Publications
Thermal proteome profiling (TPP) provides a powerful approach to studying proteome-wide
interactions of small therapeutic molecules and their target and off-target proteins …

Horizontal cell biology: monitoring global changes of protein interaction states with the proteome-wide cellular thermal shift assay (CETSA)

L Dai, N Prabhu, LY Yu, S Bacanu… - Annual review of …, 2019 - annualreviews.org
The cellular thermal shift assay (CETSA) is a biophysical technique allowing direct studies of
ligand binding to proteins in cells and tissues. The proteome-wide implementation of CETSA …

The GOLIATH project: Towards an internationally harmonised approach for testing metabolism disrupting compounds

J Legler, D Zalko, F Jourdan, M Jacobs… - International Journal of …, 2020 - mdpi.com
The purpose of this project report is to introduce the European “GOLIATH” project, a new
research project which addresses one of the most urgent regulatory needs in the testing of …

Target identification and validation of natural products with label-free methodology: A critical review from 2005 to 2020

L Dai, Z Li, D Chen, L Jia, J Guo, T Zhao… - Pharmacology & …, 2020 - Elsevier
Natural products (NPs) have been an important source of therapeutic drugs in clinic use and
contributed many chemical probes for research. The usefulness of NPs is however often …

Development of new approach methods for the identification and characterization of endocrine metabolic disruptors—a PARC project

A Braeuning, P Balaguer, W Bourguet… - Frontiers in …, 2023 - frontiersin.org
In past times, the analysis of endocrine disrupting properties of chemicals has mainly been
focused on (anti-) estrogenic or (anti-) androgenic properties, as well as on aspects of …

[HTML][HTML] The glyphosate formulation Roundup® LB plus influences the global metabolome of pig gut microbiota in vitro

JL Krause, SB Haange, SS Schäpe… - Science of the Total …, 2020 - Elsevier
Glyphosate is the world's most widely used herbicide, and its potential side effects on the
intestinal microbiota of various animals, from honeybees to livestock and humans, are …