Enabling protein degradation with small-molecule drugs has emerged as an innovative approach to the development of therapeutics against otherwise intractable targets. Two landmark studies that established the therapeutic potential of heterobifunctional degrader molecules are celebrating their 10-year anniversary...
There are 80 FDA-approved therapeutic agents that target about two dozen different protein kinases and seven of these drugs were approved in 2023. Of the approved drugs, thirteen target protein-serine/threonine protein kinases, four are directed against dual specificity protein kinases (MEK1/2), ...
Throughout history, many small-molecule drugs have contributed to medical progress and improved the lives of patients (Fig. 2). Some of these early drugs are still in use today, whereas others have disappeared from the market, but were instrumental in paving the way for improved treatments in...
small-molecule drugstailor-made amino acidsAmino acids (AAs) play an important role in the modern health industry as key synthetic precursors for pharmaceuticals, biomaterials, biosensors, and drug delivery systems. Currently, over 30% of small-molecule drugs contain residues of tailor-made AAs or ...
The discovery of new inflammatory pathways and the mechanism of action of inflammatory, autoimmune, genetic, and neoplastic diseases led to the development of immunologically driven drugs. We aimed to perform a narrative review regarding the rising of a new class of drugs capable of blocking importan...
Small molecule APIs include vitamin C, steroids, and aminoglycoside and beta-lactam antibiotics. Polymeric resins play an important role in purifying generic drugs and custom APIs. Resins can be used in adsorption mode or in ion exchange chromatography columns to: Purify raw materials Remove ...
ABBV-CLS-484 is a PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. Here we have explored the therapeutic potential of a related small-molecule-inhibitor, Compound-182. We demonstrate that Compound-182 is a highly potent and selective active site competitive inhibitor of PTP1B and ...
Small molecule drugs are easy to deliver and safe to use on bedside since most of them are long been scrutinized by supervising agencies and worldwide market25. Many classical drugs have been found a novel target in recent years, bringing new hope to some refractory diseases. Therefore, we ...
where small molecule applications contribute to more than half of specialty sales. For instance, as reported by the U.S. Food and Drug Administration (FDA) in 2022, small molecules held around 59% of new drug approvals, representing 22 of the 37 new drugs approved in 2022 were small molecu...
molecule structures capable of forming hydrogen bonds with the Cys108-NH of the TNIK hinge region. Targeting less-conserved adjacent allosteric pockets (such as a hydrophobic back cavity close to the gatekeeper residue) in addition to the active site can achieve better selectivity of the lead ...