2018
DOI: 10.1101/423061
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Comparative analysis of PknB inhibitors for reactivity and toxicity

Abstract: Bacterial serine/threonine kinases are increasingly sought after as drug targets for new antibiotics.PknB, an essential kinase in Mycobacteria tuberculosis, is intensely targeted, and many inhibitors are in the developmental pipeline. These inhibitors typically are derived from screens of known kinase inhibitors and most share similar chemical properties as their parent compounds were all designed for optimal pharmacokinetic properties in the human body. Here, we investigate the reactivity and toxicity of a pr… Show more

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“…Although mouse models would be premature at this stage of development, a small medium-throughput animal model may help prioritize compounds to advance to later testing stages. Zebrafish (Danio rerio) have a kinome with a median catalytic domain identity of 75% to the human kinome, allowing it to be used as an accurate model for kinase inhibitor toxicity . Since the embryos develop rapidly, most kinases are also expressed and active, providing the largest possible pool to assess for side effects.…”
mentioning
confidence: 94%
“…Although mouse models would be premature at this stage of development, a small medium-throughput animal model may help prioritize compounds to advance to later testing stages. Zebrafish (Danio rerio) have a kinome with a median catalytic domain identity of 75% to the human kinome, allowing it to be used as an accurate model for kinase inhibitor toxicity . Since the embryos develop rapidly, most kinases are also expressed and active, providing the largest possible pool to assess for side effects.…”
mentioning
confidence: 94%