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Showing 1–12 of 12 results
Advanced filters: Author: Matthew B Robers Clear advanced filters

  • Tracers are fluorescent protein ligands required for various displacement assays. Here, the authors announce a curated database named tracerDB, which will make essential tracer data, contributed by the worldwide research community, easily available and searchable.

    • Johannes Dopfer
    • James D. Vasta
    • Martin P. Schwalm
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-5

  • Drug molecules operate through physical interaction with specific cellular targets, and understanding this interaction is important for mechanisms and the potential therapeutic effect of drug candidates. Here, the authors show that bioluminescence resonance energy transfer can be used to monitor the intracellular engagement of a drug with its target.

    • Matthew B. Robers
    • Melanie L. Dart
    • Keith V. Wood
    ResearchOpen Access
    Nature Communications
    Volume: 6, P: 1-10

  • The use of NMR spectroscopy and development of a cellular BRET KRAS engagement assay revealed that noncovalent ligands can access the switch-II pocket of KRAS hotspot mutants.

    • James D. Vasta
    • D. Matthew Peacock
    • Kevan M. Shokat
    ResearchOpen Access
    Nature Chemical Biology
    Volume: 18, P: 596-604

  • Cyclin-dependent kinase (CDK) inhibitors are widely used both in the clinic and for basic research aimed at dissecting the specific cellular functions of specific CDKs. Here, the authors report the development of a panel of fluorescent reporter probes and provide a comprehensive profile of the inhibitory activity of several CDK inhibitors towards all 21 CDKs in living cells.

    • Carrow I. Wells
    • James D. Vasta
    • Matthew B. Robers
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-11

  • Owens et al. reported PFI-7, a selective and potent antagonist of GID4 of the CTLH E3 ligase complex, which enables identification of human GID4 targets. This study provides valuable insights into GID4 functions and a powerful tool for advancing new targeted protein degradation strategies.

    • Dominic D. G. Owens
    • Matthew E. R. Maitland
    • Cheryl H. Arrowsmith
    Research
    Nature Chemical Biology
    Volume: 20, P: 1164-1175

  • Development of a paralog-hopping approach leveraging chemical proteomic data on covalently liganded cysteines revealed an allosteric pocket shared by cysteine-containing and cysteine-less paralogous cyclin E proteins.

    • Yuanjin Zhang
    • Zhonglin Liu
    • Benjamin F. Cravatt
    Research
    Nature Chemical Biology
    Volume: 21, P: 420-431

  • Murray et al. identified and characterized a small-molecule inhibitor of human COQ8A, which belongs to the UbiB protein family and is essential for coenzyme Q biosynthesis.

    • Nathan H. Murray
    • Christopher R. M. Asquith
    • David J. Pagliarini
    Research
    Nature Chemical Biology
    Volume: 19, P: 230-238

  • A highly selective inhibitor of the DCLK1/2 kinases is used to uncover the consequences of DCLK1 inhibition on viability, phosphosignaling and the transcriptome in patient-derived organoid models of pancreatic ductal adenocarcinoma.

    • Fleur M. Ferguson
    • Behnam Nabet
    • Nathanael S. Gray
    Research
    Nature Chemical Biology
    Volume: 16, P: 635-643

  • Structural insights demonstrating small-molecule-mediated dimerization of BRD4 bromodomains led to the development of biBET, a compound that potently inhibits BRD4–acetyl-lysine interactions by bivalent binding to tandem bromodomains.

    • Michael J Waring
    • Huawei Chen
    • Yi Yao
    Research
    Nature Chemical Biology
    Volume: 12, P: 1097-1104

  • Bioluminescence resonance energy transfer, from the substrate of a luciferase fused with a G protein–coupled receptor to a fluorescent dye covalently linked to a receptor ligand, allows the profiling of ligand affinity and binding kinetics.

    • Leigh A Stoddart
    • Elizabeth K M Johnstone
    • Kevin D G Pfleger
    Research
    Nature Methods
    Volume: 12, P: 661-663