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Pharmaceuticals, Volume 13, Issue 2 (February 2020) – 15 articles
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Cover Story (view full-size image) Targeting deregulation within cancer cell metabolism appears to be promising strategy for the [...] Read more. Targeting deregulation within cancer cell metabolism appears to be promising strategy for the development of more efficient cancer treatments. Recent reports highlight the crucial role of the serine synthetic pathway, and particularly of its first enzyme, the phosphoglycerate dehydrogenase (PHGDH), in sustaining cancer progression. Yet, due to the usually too weak potencies in cell-based settings, the inhibitors reported so far failed to identify the potential of this approach. In this paper, we report the structure-activity relationships of a series of α-ketothioamides that we recently identified. The activity of the more potent compounds was confirmed by cellular thermal shift assays and cell-based experiments. The findings provide a deeper understanding of this series and to the identification of new PHGDH inhibitors. View this paper.