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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.

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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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Biophysics

Sygnature Discovery

Comprehensive Assay Development for Diverse Applications Our team here at Sygnature Discovery, comprised of expert biophysicists, is highly experienced in a variety of target classes and drug modalities. Sygnature Discovery’s Biophysical Assay Development Capabilities: 1.

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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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Variability in biological activity measurements reported in the drug discovery literature

Molecular Design

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 biophysical assays tend to be favored for screening fragments).