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The superfamily of the protein kinase C (PKC) comprises ten isozymes and is widely known for its key role in signal transduction. Acquiring isozyme-selective inhibitors is a difficult task due to the high sequence similarity within the ten PKCs. It was found that N-(4-acetylphenyl)-3-amino-6,7-ethelendioxy-thieno[2,3-b]quinoline-2-carboxamide (1b) shows promising inhibitory activities on the interaction of PKCε with its adaptor protein, the receptor for activated C-kinase 2 (RACK2), hence interfering with PKCε signaling. A structural isomer of (1a metha-acetyl), compound (1b para-acetyl) was found to exhibit in addition to strong inhibitory activity on PKCε signaling with IC50 4.25 µM also anti-angiogenic activities. The quinolines without thiophene ring as a “open” analogs of 1b were inactive in primary assays.
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