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Structure-Based Optimization of Covalent, Small-Molecule Stabilizers of the 14-3-3?/ER? Protein–Protein Interaction from Nonselective Fragments

Covalent Modifiers

3c05161 The stabilization of protein–protein interactions (PPIs) has emerged as a promising strategy in chemical biology and drug discovery. Here, we show the structure-based optimization of the nonselective fragment toward selective and highly potent small-molecule stabilizers of the 14-3-3σ/ERα complex.

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Site-Specific Molecular Glues for the 14-3-3/Tau pS214 ProteinProtein Interaction via Reversible Covalent Imine Tethering

Covalent Modifiers

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.

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Location-agnostic site-specific protein bioconjugation via Baylis Hillman adducts

Covalent Modifiers

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.

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

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.

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Biophysics

Sygnature Discovery

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.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

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.