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Showing 1–13 of 13 results
Advanced filters: Author: Nicola A Burgess-Brown Clear advanced filters

  • SPNS2 exports S1P and FTY720-P to control immune cell migration. Here, the authors use cryo-EM, immunofluorescence, in vitro binding and in vivo S1P export, and MD simulations to uncover the mechanisms of SPNS2’s transport and inhibition.

    • Huanyu Z. Li
    • Ashley C. W. Pike
    • David B. Sauer
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-14

  • ELOVLs are membrane-embedded enzymes that elongate very long chain fatty acids, precursors of sphingolipids and ceramides. The first crystal structure of a human ELOVL reveals an unexpected reaction mechanism, suggesting potential approaches for inhibition in disease.

    • Laiyin Nie
    • Tomas C. Pascoa
    • Elisabeth P. Carpenter
    Research
    Nature Structural & Molecular Biology
    Volume: 28, P: 512-520

  • The X-ray crystal structure of the potassium channel TASK-1 reveals the presence of an X-gate, which traps small-molecule inhibitors in the intramembrane vestibule and explains their low washout rates from the channel.

    • Karin E. J. Rödström
    • Aytuğ K. Kiper
    • Elisabeth P. Carpenter
    Research
    Nature
    Volume: 582, P: 443-447

  • TMEM16K is a member of the TMEM16 family of integral membrane proteins that are either lipid scramblases or chloride channels. Here the authors combine cell biology, electrophysiology measurements, X-ray crystallography, cryo-EM and MD simulations to structurally characterize TMEM16K and show that it is an ER-resident lipid scramblase.

    • Simon R. Bushell
    • Ashley C. W. Pike
    • Elisabeth P. Carpenter
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-16

  • X-ray crystallographic analyses of KDM5B provide a view of the enzyme's iron(II)- and 2-oxoglutarate-containing catalytic core, and structures of KDM5B complexes with small-molecule inhibitors reveal selectivity profiles for multiple compound chemotypes.

    • Catrine Johansson
    • Srikannathasan Velupillai
    • Udo Oppermann
    Research
    Nature Chemical Biology
    Volume: 12, P: 539-545

  • Here, Chi et al. report cryo-EM structures of the human Kv3.1a channel, revealing a unique arrangement of the cytoplasmic T1 domain, which allows the interactions with the C-terminal axonal targeting motif and key components of the gating machinery. These findings provide insights into the functional relevance of previously unknown interdomain interactions in Kv3 channels and may guide the design of new pharmaceutical drugs.

    • Gamma Chi
    • Qiansheng Liang
    • Katharina L. Dürr
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-15

  • The cryo-EM structure of human polycystin-2 (PC2) in a closed conformation reveals a domain located above the pore filter, forming an upper vestibule and making contacts with the pore and voltage-sensor-like domains.

    • Mariana Grieben
    • Ashley C W Pike
    • Elisabeth P Carpenter
    Research
    Nature Structural & Molecular Biology
    Volume: 24, P: 114-122

  • The European Lead Factory combines assets and experience from major pharma with innovation and agility of academia and SMEs in a collaborative platform to expand access to high-throughput screening. With many successes heading towards the clinic, the organization is broadening its approach to screening and partnering.

    • Philip S. Jones
    • Sylviane Boucharens
    • Jon S. B. de Vlieger
    Comments & Opinion
    Nature Reviews Drug Discovery
    Volume: 21, P: 245-246

  • The Innovative Medicines Initiative Consortium RESOLUTE has started to develop tools and produce data sets to de-orphanize transporters in the solute carrier protein (SLC) superfamily, thereby lowering the barrier for the scientific community to explore SLCs as an attractive drug target class.

    • Giulio Superti-Furga
    • Daniel Lackner
    • Claire M. Steppan
    Comments & Opinion
    Nature Reviews Drug Discovery
    Volume: 19, P: 429-430

  • Target 2035 aims to develop a potent and selective pharmacological modulator for every human protein by 2035 with the results made publicly available. This Roadmap article sets out how that will be achieved.

    • Aled M. Edwards
    • Dafydd R. Owen
    • Suzanne Ackloo
    Reviews
    Nature Reviews Chemistry
    Volume: 9, P: 634-645

  • Mapping multiple glycan species to the same peptide and location from shared retention time of glycopeptides with MS and HPLC, Chalk, Greenland et al. construct a detailed mass-retention time database for Spike protein glycopeptides. This allows any mass LC-MS laboratory to reliably identify and quantify Spike protein glycopeptides from a single overnight elastase protein digest in less than 90 minutes.

    • Rod Chalk
    • William E. P. Greenland
    • Nicola A. Burgess-Brown
    ResearchOpen Access
    Communications Biology
    Volume: 4, P: 1-8

  • A genetics-led translational approach integrating functional genomic predictors, knowledge of network connectivity and immune ontologies defines the drug target prioritization landscape for 30 immune traits at the gene and pathway level.

    • Hai Fang
    • Georg Beckmann
    • Julian C. Knight
    Research
    Nature Genetics
    Volume: 51, P: 1082-1091