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(NPS) and ‘new synthetic substances’ appeared in 2008 to describe a range of diverse substances that mimic the effects of various illegal substances (ecstasy, amphetamines, cocaine, cannabis, etc.). Other terms used such as designer drugs, research chemicals (RC) and legal highs respectively allude to their imitative aspect, the fact that they are artificially synthesised and their legal status...
The binding mechanism of a new class of lipid-competitive, ATP non-competitive, p110α isoform-selective PI3K (phosphoinositide 3-kinase) inhibitors has been elucidated. Using the novel technique of isoform reciprocal mutagenesis of non-conserved amino acids in the p110α and p110β isoforms, we have identified three unique binding mechanisms for the p110α-selective inhibitors PIK-75, A-66S and J-...
A novel inhibitor of topoisomerases designated as topostatin was isolated from the culture filtrate of Thermomonospora alba strain No. 1520. Topostatin inhibited the relaxation of supercoiled pBR322 DNA by calf thymus topoisomerase I, and also inhibited the relaxation of supercoiled pBR322 DNA and decatenation of kinetoplast DNA by human placenta topoisomerase II. Topostatin had neither ability...
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