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Showing 1–12 of 12 results
Advanced filters: Author: Christian Ottmann Clear advanced filters

  • Targeting transcription factors with small molecules remains a significant challenge in drug discovery. Here, the authors present a structure-based approach to stabilize ChREBPα/14-3-3 interactions, suppressing ChREBPβ and protecting β-cells from glucolipotoxicity, showcasing ‘molecular glues’ as tools to control difficult to target transcription factors.

    • Liora S. Katz
    • Emira J. Visser
    • Donald K. Scott
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-16

  • Molecular glues have great potential for drug discovery if they can be systematically discovered. Konstantinidou, et al describe a scaffold-hopping approach using multicomponent reaction chemistry to design molecular glues that induce 14-3- 3σ/ERα formation in cells.

    • Markella Konstantinidou
    • Marios Zingiridis
    • Michelle R. Arkin
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-13

  • Mutations in the chloride channel CFTR that impair plasma membrane insertion and ion transport are the cause of cystic fibrosis. Here, the authors identify a macrocycle that stabilizes the interaction of mutant CFTR with the chaperone-like protein 14-3-3 and rescues its biological function.

    • Loes M. Stevers
    • Madita Wolter
    • Christian Ottmann
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-9

  • Small molecule stabilizers of protein–protein interactions hold great therapeutic potential. Based on virtual screening and molecular docking, the authors here develop a strategy to evolve weak, promiscuous inhibitors of 14-3-3 interactions into selective stabilizers of the 14-3-3/ChREBP complex.

    • Eline Sijbesma
    • Emira Visser
    • Christian Ottmann
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-9

  • A molecular tweezer has been shown to bind to the surface of a 14-3-3 protein through a particular lysine residue. This interaction — characterized in detail by protein crystallography and computational modelling — disrupts the protein's binding with partner proteins. These findings ascertain supramolecular chemistry as an enticing tool in chemical biology, here towards modulating protein functions.

    • David Bier
    • Rolf Rose
    • Christian Ottmann
    Research
    Nature Chemistry
    Volume: 5, P: 234-239

  • The combination of a covalent electrophile with a peptide or protein-based scaffold enables the targeting of shallow protein surfaces, but the approaches to convert native peptide sequences into covalent binders are missing. Here, the authors report the design of protein-based thiomethacrylate ester electrophiles that can be installed on unprotected peptides and proteins via cysteine side chains and react efficiently and selectively with cysteine and lysine side chains on the target.

    • Ronen Gabizon
    • Barr Tivon
    • Nir London
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-16

  • Upon the binding of small ligands, nuclear receptors regulate the transcription of genes that are associated with a number of disease mechanisms. Here, the authors report on a novel allosteric ligand binding site on the nuclear receptor RORγt.

    • Marcel Scheepstra
    • Seppe Leysen
    • Luc Brunsveld
    ResearchOpen Access
    Nature Communications
    Volume: 6, P: 1-10

  • The authors show that binding of 14-3-3ζ enhances cytosolic Tau solubility by promoting phosphorylated Tau removal from microtubules, while simultaneously inhibiting Tau aggregation both directly and indirectly via suppression of condensate formation.

    • Janine Hochmair
    • Maxime C. M. van den Oetelaar
    • Susanne Wegmann
    ResearchOpen Access
    Communications Biology
    Volume: 8, P: 1-17

  • Synthetic peptide libraries can access broad chemical space, but generally examine only ~ 106 compounds. Here, the authors show that in-solution affinity selection, interfaced with nLC-MS/MS sequencing, can identify binders from fully randomized synthetic libraries of 108 members.

    • Anthony J. Quartararo
    • Zachary P. Gates
    • Bradley L. Pentelute
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-11

  • Mineralized collagen is the building block of bone but how the collagen directs hydroxyapatite formation remains unclear. Here, the authors demonstrate cylindrical pores in collagen and how the anisotropic growth of hydroxyapatite directs the orientation of crystal growth in mineralized collagen.

    • YiFei Xu
    • Fabio Nudelman
    • Nico Sommerdijk
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-12