Covalent Modifiers

FEBRUARY 1, 2024

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.

Biophysical Assays 200

Biophysical Assays Small Molecule Drug Development Production 200

Covalent Modifiers

SEPTEMBER 9, 2023

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.

Small Molecule 200

Small Molecule Biophysical Assays Production Drugs 200

Drug Target Review

NOVEMBER 1, 2023

We support the drug discovery projects of the CCDD with assay development and screening, biophysics, structural biology and recombinant protein production. The team that I lead within the CCDD is called the Hit Discovery and Structural Design Team.

Fragment Screening 96

Fragment Screening Biochemical Assays Small Molecule Biophysical Assays 96

Drug Target Review

JANUARY 16, 2025

However, close to 40 percent of all macrocyclic drugs are orally bioavailable, 6 including natural products and derivatives thereof that have provided chemical structure clues with respect to permeability. 12 Ring bridging strategies have also been effective in addressing permeability, as seen with MK-0616.

Drug Development 52

Drug Development Small Molecule Drugs FDA Approval 52