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  • An INSPIRE platform for therapeutic regulators and sensors, based on split human domains binding physiological or clinically approved compounds, has been developed and demonstrated on several human proteins in a relevant ligand concentration range.

    • Erik Rihtar
    • Tina Lebar
    • Roman Jerala
  • Single-molecule methods are a powerful tool to study the kinetics of ATP-powered enzymes. A method that locally controls the generation of ATP significantly increases the throughput of single-molecule approaches and unlocks single-turnover analysis of molecular machines.

    • Jens C. Schmidt
    News & Views
  • Artificial intelligence (AI) is poised to transform therapeutic science. Therapeutics Data Commons is an initiative to access and evaluate AI capability across therapeutic modalities and stages of discovery, establishing a foundation for understanding which AI methods are most suitable and why.

    • Kexin Huang
    • Tianfan Fu
    • Marinka Zitnik
  • Compound library screening combined with medicinal chemistry and structural biology approaches enables the development of potent and highly selective cell-permeable small-molecule inhibitors of phosphatidylinositol 3-kinase C2α activity and function.

    • Wen-Ting Lo
    • Hassane Belabed
    • Volker Haucke
    Article Open Access
  • Isoform-selective inhibition of JAK kinases is of key interest in drug discovery. A novel pocket in the JAK pseudokinase domain was targeted by an allosteric covalent inhibitor, leading to specific JAK1 inhibition and providing a deeper understanding of cytokine signaling.

    • Olli Silvennoinen
    • Teemu Haikarainen
    • Anniina Virtanen
    News & Views