Covalent Modifiers

SEPTEMBER 9, 2023

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. Orthogonal biophysical assays, including mass spectrometry and fluorescence anisotropy, were used to establish structure–activity relationships.

Small Molecule 200

Small Molecule Biophysical Assays Production Drugs 200

Covalent Modifiers

FEBRUARY 1, 2024

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.

Biophysical Assays 200

Biophysical Assays Small Molecule Drug Development Production 200

Drug Target Review

NOVEMBER 1, 2023

The mission of the CCDD is to discover novel small-molecule therapeutics for the treatment of cancer and progress them to hypothesis testing phase 1 clinical trials. We support the drug discovery projects of the CCDD with assay development and screening, biophysics, structural biology and recombinant protein production.

Fragment Screening 96

Fragment Screening Biochemical Assays Small Molecule Biophysical Assays 96

Drug Target Review

JANUARY 16, 2025

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. What are macrocycles and why are they interesting for drug discovery?

Drug Development 52

Drug Development Small Molecule Drugs FDA Approval 52