Cluster of differentiation 20 (CD20) is a nonglycosylated, multispanning transmembrane protein specifically integrated by B lymphocytes. Similar to CD20, another four-pass transmembrane protein, claudin 18.2, has attracted attention as an emerging therapeutic target for cancer.
View Article and Find Full Text PDFImmunotherapy has led to a paradigm shift in the treatment of cancer. Current cancer immunotherapies are mostly antibody-based, thus possessing advantages in regard to pharmacodynamics (., specificity and efficacy).
View Article and Find Full Text PDFProtein Expr Purif
March 2023
CD1E, one of the most important glycolipid antigens on T cell membranes, is required for glycolipid antigen presentation on the cell surface. Cell-based recombinant expression systems have many limitations for synthesizing transmembrane proteins such as CD1E, including low protein yields and miss folding. To overcome these challenges, here we successfully synthesized high-quality soluble CD1E using an E.
View Article and Find Full Text PDFA copper-mediated decarboxylative coupling reaction of 3-indoleacetic acids with pyrazolones was described. This protocol realized new functionalization of pyrazolones under simple reaction conditions and exhibited high functional group compatibility and broad substrate scope. Notably, the products displayed antiproliferative activity against cancer cells.
View Article and Find Full Text PDFHerein, we describe an efficient and benign protocol for direct C-3 sulfonylmethylation of imidazo[1,2-]pyridines with glyoxylic acid and sodium sulfinates. Various sulfonylmethylated imidazo[1,2-]pyridines were synthesized in water under transition metal catalyst-free conditions. This multicomponent reaction featured available substrates, good functional group tolerance, moderate to excellent yields, and mild reaction conditions.
View Article and Find Full Text PDFA series of KRAS G12C-targeting PROTACs (PROteolysis TArgeting Chimeras) were designed and synthesized based on KRas G12C-IN-3 (a KRAS G12C inhibitor) and pomalidomide as degraders of KRAS G12C with a molecular weight of < 900. Among them, compound KP-14 (m.w.
View Article and Find Full Text PDFA copper-mediated decarboxylative coupling reaction between arylacetic acids and 1,3-dicarbonyl compounds was described. Significantly, methanocycloocta[]indoles were also obtained by sequential intramolecular dehydrocyclization process in some cases. This protocol featured a broad substrate scope, simple operations, and good yields.
View Article and Find Full Text PDFA copper-catalyzed C-3 functionalization of imidazo[1,2-]pyridines with 3-indoleacetic acids through an aerobic oxidative decarboxylative process has been developed. The protocol provided a series of 3-(1-indol-3-ylmethyl)-imidazo[1,2-]pyridines in moderate to good yields under simple reaction conditions. Importantly, some products exhibited potent antiproliferative activity in cancer cell lines.
View Article and Find Full Text PDFHerein, we describe the novel reactivity of hexafluoroisopropyl 2-aminobenzoates. The metal-free synthesis of 1,4-benzodiazepines and quinazolinones from hexafluoroisopropyl 2-aminobenzoates has been developed at room temperature. These procedures feature good functional group tolerance, mild reaction conditions, and excellent yields.
View Article and Find Full Text PDFHerein, we present a copper-mediated decarboxylative sulfonylation of arylacetic acids with sodium sulfinates that provides viable access to sulfone compounds. This protocol features readily available feedstocks, simple operations, high regioselectivities, and moderate to good yields. The newly obtained products could be converted to other useful compounds.
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