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 …
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 …
Proteome integral solubility alteration: a high-throughput proteomics assay for target deconvolution
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 …
physicochemical properties of proteins in cell lysates, living cells, and organisms. These …
Nonparametric analysis of thermal proteome profiles reveals novel drug-binding proteins
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) …
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 …
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)
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 …
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
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 …
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 …
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 …
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
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 …
intestinal microbiota of various animals, from honeybees to livestock and humans, are …