Chromopynones
WebWe show that chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3, inhibits cancer cell growth and promises to inspire new drug discovery programmes aimed at tumour metabolism. Metadata. Authors/Creators: Karageorgis, ... To design a representative pseudo NP class we considered basic guidelines that we expect to be applicable in a general sense. First, because chirality is a defining property of many NPs, and stereogenic content correlates with bioactivity19,20, it was planned to combine NP fragments in a novel three-dimensional … See more To compare the chemical space occupied by the chromopynones, NP-likeness scores, as introduced in ref. 23 (Fig. 3a and Supplementary … See more Pseudo NPs may display bioactivities that are very different from those of the individual guiding NPs from which the newly combined fragments were derived. Therefore, this chemocentric approach requires a wider … See more Selectivity for inhibition of the two most cancer-relevant glucose transporters, GLUT-1 and -340,41, was assessed with human colorectal adenocarcinoma DLD-1 cells, which mainly express GLUT-1 and GLUT-3 (as reported … See more For inhibition of glucose uptake by the chromopynones a clear structure–activity relationship emerged. Thus, the substitution pattern around the fused phenyl ring was important for activity and potency (Table 1, … See more
Chromopynones
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WebSep 13, 2024 · Chromopynones were subjected to a broad biological investigation employing phenotypic assays, since their bioactivity could not be predicted. This investigation led to the discovery that a few analogues were inhibiting glucose uptake by cancerous tissue. Subsequent investigation also revealed that the most potent … WebWe show that chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3, inhibits cancer cell growth and promises to inspire new drug discovery programmes aimed at tumour metabolism. Related: SLC2A1 Cancer Prevention and Risk Reduction Feitosa SG, Viana KF, Luna ECM, et al.
WebTo arrest these trends, the logic of seeking new bioactive agents with enhanced natural mimicry is considered; notably that molecules constructed by proteins (enzymes) are more likely to interact with other proteins (e.g., targets and transporters), a notion validated by natural products.
WebJan 1, 2024 · Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and-3. Nat. Chem. (2024) W. Fan et al. Glucose-responsive sequential generation of hydrogen peroxide and nitric oxide for synergistic cancer starving-like/gas therapy. Angew. Chem. WebNov 1, 2024 · We show that chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3, inhibits cancer cell growth …
WebWe show that chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3, inhibits cancer cell growth and promises to …
WebChromopynones selectively inhibit glucose uptake in cells; however, other compounds that contain only either the chromane or THPM fragments did not inhibit glucose uptake. 122 … flower town hotel and spaWebColorless polyimides (CPIs) with outstanding mechanical properties are essential materials in the production of flexible display panels, foldable windows, and even spacecraft cockpits. This paper specifically elaborates that the Morkit unit, and azo and nitro chromophores are important factors contributing to yellow PI, together with the well-known charge transfer … green building programs usaWebDec 17, 1973 · Reversible dissociation of the purple complex in bacteriorhodopsin and identification of 13-cis and all-trans-retinal as its chromophores flower town hotel rabatWebchromopynones define a truly novel, structurally unprecedented glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and … green building program ymcaWebChromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3 New natural-product-inspired molecules are often limited by … green building program canadaWebOf the molecules found, >75% have not been described previously; 20% of the compounds exhibit novel scaffolds. Their structural and physicochemical properties comply with established rules of drug- and fragment-likeness and exhibit increased structural complexities compared to synthetically produced fragments. flower town hotel \u0026 spa rabatWebOct 3, 2024 · Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3 New natural-product-inspired molecules are often limited by their only partial... flower town in forest art