Covalent Modifiers

FEBRUARY 10, 2025

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.

Biophysical Assays 173

Biophysical Assays Small Molecule Engineering Regulations 173

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

APRIL 7, 2025

Advancements in screening technologies for small-molecule drug discovery including cellular assays, computational screening, and biophysics-based methods enhanced by structural biology breakthroughs have improved screening hit rates and facilitated the identification of drug candidates for previously undruggable targets.

Fragment Screening 52

Fragment Screening Drugs Small Molecule Biophysical Assays 52

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 have several exciting projects in various stages of discovery, but a small-molecule drug that is causing a lot of excitement at the moment is Capivasertib.

Fragment Screening 96

Fragment Screening Biochemical Assays Small Molecule Biophysical Assays 96

Sygnature Discovery

JUNE 17, 2024

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.

Biophysical Assays 52

Biophysical Assays Screening Hits Assay Development Fragment Screening 52

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