Identification of Small-Molecule Noncovalent Binders Utilizing SAMDI Technology

High-Throughput Screening of Small Molecule Libraries using SAMDI Mass Spectrometry

High-throughput screening is a common strategy used to identify compounds that modulate biochemical activities, but many approaches depend on cumbersome fluorescent reporters or antibodies and often produce false-positive hits. The development of "label-free" assays addresses many of these limitations, but current approaches still lack the throughput needed for applications in drug discovery. T...

PriaXplore® - a novel technology platform for the identification of small molecule modulators of protein-protein interactions

Protein-protein interactions (PPIs) are broadly recognized as an emerging target class for a whole new era in drug discovery. They show significant differences to classical target classes and have been regarded as “undruggable” for a long time. Priaxon AG has developed a unique, proprietary technology platform for PPI drug discovery. PriaXplore employs novel computational and synthetic approach...

Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalysts.

Catalysis by neutral, organic, small molecules capable of binding and activating substrates solely via noncovalent interactions--particularly H-bonding--has emerged as an important approach in organocatalysis. The mechanisms by which such small molecule catalysts induce high enantioselectivity may be quite different from those used by catalysts that rely on covalent interactions with substrates...

Modeling of Human Prokineticin Receptors: Interactions with Novel Small-Molecule Binders and Potential Off-Target Drugs

BACKGROUND AND MOTIVATION The Prokineticin receptor (PKR) 1 and 2 subtypes are novel members of family A GPCRs, which exhibit an unusually high degree of sequence similarity. Prokineticins (PKs), their cognate ligands, are small secreted proteins of ∼80 amino acids; however, non-peptidic low-molecular weight antagonists have also been identified. PKs and their receptors play important roles und...

Identification of Small Molecule Inhibitors of Pre - mRNA