With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets. Covalent drugs have the potential to provide enhanced potency and prolonged duration of action compared to non-covalent drugs. Emerging areas of interest include the development of reversible covalent inhibitors, covalent degraders, and covalent targeting of non-cysteine amino …Read More >

RNA-targeted therapeutics are highly intriguing due to their unique physiological properties and novel modes of action in drug R&D. Developing methods to target RNA can lead to new therapeutic options, especially for conditions where RNA plays a pivotal role, such as genetic disorders, viral infections, and cancer. Over the past decade, discovering novel chemical matter …Read More >

Bromodomain and extra-terminal domain (BET) family proteins are key regulators of gene transcription and have been implicated in a wide range of diseases, making these proteins a potential therapeutic target.  Abnormal BET protein activity has been linked to cancer, inflammatory disorders, viral infections, and neurodegenerative conditions. In a recent publication, researchers highlight the discovery of …Read More >

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug, several new strategies have recently become available for targeting the mutant protein. One of the most promising of these involves the use of low molecular weight compounds that promote refolding and reactivation of mutant p53 …Read More >

Introduction: Molecular glues (MGs) are a class of small molecules that alter the surface properties of proteins to strengthen or induce protein-protein interactions (PPI), leading to specific biological effects like protein degradation, pathway inhibition, or activation. Their unique properties endow them with high selectivity and bioavailability, allowing for controlled drug release. Molecular glues show great …Read More >

Glucagon‐like peptide‐1 (GLP-1) receptor agonists have emerged as promising therapeutic options for addressing type‐2 diabetes, obesity, and related conditions. However, because of the continued need for injectable administration, many GLP-1 agonists face compliance challenges. To improve the design and production of GLP-1 receptor biased agonists with enhanced druggability, a novel small molecule, designated SAL0112, was …Read More >

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred to as targeted covalent inhibitors (TCIs).  In this webinar, experts discuss innovative approaches to screen for covalent binders, strategies for the synthesis of covalent warheads, and assays to optimize the ADME/DMPK properties of these molecules. …Read More >

Casein kinase 2-interacting protein-1 (CKIP-1) performs a critical negative role in the regulation of bone formation. Accumulated evidence strongly supports CKIP-1 as an attractive therapeutic target in osteoporosis.  As a scaffold protein lacking enzymatic activity, CKIP-1 seems to be an undruggable target, and the development of selective small molecule inhibitors targeting CKIP-1 has proven to …Read More >

The heme oxygenase (HO) family comprises the major isozymes HO-1 and HO-2, of which HO-1 is deemed as an emerging target for cancer therapy. HO-1 overexpression is often observed in prostate, renal, colon, lung, breast, and glioma cancers. In a publication in ACS Med Chem Letters, WuXi AppTec scientists report the discovery of five series …Read More >