Small Molecules Archives

Discovery of a Novel Covalent Inhibitor Using DEL

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets. Covalent drugs...

DEL Screening to Discover Small Molecule Ligands for RNA

RNA-targeted therapeutics are highly intriguing due to their unique physiological properties and novel modes of action in drug R&D. Developing...

Discovery of a Selective BET Inhibitor for Treating Osteoarthritis

Bromodomain and extra-terminal domain (BET) family proteins are key regulators of gene transcription and have been implicated in a wide...

Small Molecule Reactivator of p53 Y220C Mutant

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug,...

Molecular Glues Discovery: Challenges and Opportunities

Introduction: Molecular glues (MGs) are a class of small molecules that alter the surface properties of proteins to strengthen or...

Toxicology Profile of a Novel GLP-1 Receptor Agonist

Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However,...

Strategies for Screening and Characterizing Targeted Covalent Inhibitors

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred...

Discovery of a Specific CKIP-1 Ligand using DEL

Casein kinase 2-interacting protein-1 (CKIP-1) performs a critical negative role in the regulation of bone formation. Accumulated evidence strongly supports...

Highly Selective Novel Heme Oxygenase-1 Hits Found by DEL

The heme oxygenase (HO) family comprises the major isozymes HO-1 and HO-2, of which HO-1 is deemed as an emerging...

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