Browsing by Subject Kinase

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  • OER000000888.pdf.jpg
  • Journal article


  • Authors : Cichonska, Anna; Ravikumar, Balaguru; Allaway, Robert J (2020)

  • Despite decades of intensive search for compounds that modulate the activity of particular targets, there are currently small-molecules available only for a small proportion of the human proteome. Effective approaches are therefore required to map the massive space of unexplored compound-target interactions for novel and potent activities. Here, we carried out a crowdsourced benchmarking of predictive models for kinase inhibitor potencies across multiple kinase familie...

  • OER000002546.pdf.jpg
  • Industry article


  • Authors : Rak, Marcel (2023)

  • Salt-inducible kinases 1-3 (SIK1-3) are key regulators of the LKB1-AMPK pathway and play an important role in cellular homeostasis. Dysregulation of any of the three isoforms has been associated with tumorigenesis in liver, breast, and ovarian cancers. We have recently developed the dual pan-SIK/group I p21-activated kinase (PAK) chemical probe MRIA9. However, inhibition of p21-activated kinases has been associated with cardiotoxicity in vivo, w...