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Modulating PPIs with small molecules has gained increasing attention in drug discovery, particularly targeting the 14-3-3 protein family, which interacts with several hundred client proteins and plays a central role in cellular networks.
link] Proteins labelled site-specifically with small molecules are valuable assets for chemical biology and drug development. Nat Commun 15 , 859 (2024). The unique reactivity profile of the 1,2-aminothiol moiety of N -terminal cysteines ( N -Cys) of proteins renders it highly attractive for regioselective protein labelling.
3c05161 The stabilization of protein–protein interactions (PPIs) has emerged as a promising strategy in chemical biology and drug discovery. Orthogonal biophysicalassays, including mass spectrometry and fluorescence anisotropy, were used to establish structure–activity relationships.
The challenge of GPCR drug discovery G protein-coupled receptors (GPCRs) are one of the most desirable and challenging target classes in drug discovery, as their mutation can lead to a wide range of diseases such as cancer, cardiovascular disorders and neurological conditions.
At Sygnature Discovery, we see biophysics as a core component of drug discovery projects, which can generate data throughout the pipeline. This wealth of experience supports our broader team of over 20 scientists, each trained in at least one biophysical technology.
Biochemical assays are commonly used to assess how organic compounds impact the activity of a protein of interest (POI). Het bericht Positive Impact of Dragonfly™ Discovery in Biochemical Assay verscheen eerst op ZoBio - Drug Discovery Technology.
Could you provide an overview of your research on target directed cancer drug discovery, particularly your focus on protein lagging interactions. I work in the Centre for Cancer Drug Discovery (CCDD) at The Institute of Cancer Research in London, which is an academic drug discovery centre. 2013) 56, 2059-2073.
When examining differences between IC 50 values for the same combination of target and inhibitor it's worth bearing in mind that interference with assay read-outs tends to be more of an issue at high concentration (this is why biophysicalassays tend to be favored for screening fragments).
What are macrocycles and why are they interesting for drug discovery? Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 2 Typically, small-molecule drugs target active sites buried inside proteins. 8 Why are there not more macrocyclic drugs?
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