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Showing 1–5 of 5 results
Advanced filters: Author: Malin Lemurell Clear advanced filters
  • Targeting the interaction between transcription factor TEAD and its co-repressor VGL4 is an attractive strategy to chemically modulate Hippo signaling. Here, the authors develop a proteomimetic with stabilized tertiary structure that inhibits the TEAD:VGL4 interaction in vitro and in cells.

    • Hélène Adihou
    • Ranganath Gopalakrishnan
    • Herbert Waldmann
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-10
  • A selection-based screen has now revealed preferences in small-molecule chemotypes that bind RNA as well as preferences in the RNA motifs that bind small molecules. Analysis of these data enabled the design of a small molecule that selectively binds a non-coding microRNA and upregulates expression of vascular endothelial growth factor A.

    • Hafeez S. Haniff
    • Laurent Knerr
    • Matthew D. Disney
    Research
    Nature Chemistry
    Volume: 12, P: 952-961
  • Medicinal chemistry optimizations in the progression from hit to lead to drug candidate affect properties of small-molecule drugs such as their molecular weight and lipophilicity. This Perspective analyses the properties of orally administered small-molecule drug candidates reported in the period 2015–2022 and their corresponding hit and lead compounds, and compares them with the properties of drug candidates identified between 2000 and 2010 and their hits and leads, with the aim of improving understanding of the evolution of hit finding and optimization strategies.

    • Anita Rácz
    • Levente M. Mihalovits
    • György M. Keserű
    Reviews
    Nature Reviews Drug Discovery
    Volume: 24, P: 870-887