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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

Orthogonal biophysical assays, including mass spectrometry and fluorescence anisotropy, were used to establish structure–activity relationships. 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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Positive Impact of Dragonfly™ Discovery in Biochemical Assay

Zobio

Biochemical assays are commonly used to assess how organic compounds impact the activity of a protein of interest (POI).

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

In 2007 Dr van Montfort joined the Institute of Cancer Research (London, UK), where he holds a joint position between the Centre for Cancer Drug Discovery (CCDD) and the Division of Structural Biology.

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

Covalent Modifiers

Taken together, the protein bioconjugation toolkit that we disclose herein will contribute towards the generation of both mono and multi-labelled protein-small molecule bioconjugates for applications as diverse as biophysical assays, cellular imaging, and the production of therapeutic protein–drug conjugates.