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Showing 1–11 of 11 results
Advanced filters: Author: Stephen M. Soisson Clear advanced filters

  • A new class of antibiotics that targets bacterial lipid biosynthesis is isolated from Streptomyces platensis, and demonstrates potent in vitro and in vivo activity against Gram-positive bacteria — including methicillin-resistant Staphylococcus species.

    • Jun Wang
    • Stephen M. Soisson
    • Sheo B. Singh
    Research
    Nature
    Volume: 441, P: 358-361

  • Agonists of the orexin receptor 2 (OX2R) show promise in the treatment of narcolepsy. Cryo-EM structures of active-state OX2R bound to an endogenous peptide agonist and a small-molecule agonist suggest a molecular mechanism that rationalizes both receptor activation and inhibition.

    • Chuan Hong
    • Noel J. Byrne
    • Kaspar Hollenstein
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-11

  • Ligands that activate GPCRs generally do so by stabilizing a particular conformation of the transmembrane helices. Here, the authors reveal a distinct activation mechanism where a ligand instead stabilizes a particular intracellular loop conformation.

    • Alexander S. Powers
    • Aasma Khan
    • Ron O. Dror
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-12

  • Mutations in the IDH1 gene that generate neomorphic metabolites are linked to multiple human tumors including glioma. Here, the authors disclose novel mutant IDH1 inhibitors and contrast their mechanism and binding mode to molecules in clinical use.

    • Mark A. McCoy
    • Jun Lu
    • Christian Fischer
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-10

  • Crystallographic analysis of human O-GlcNAc hydrolase (hOGA) fragments containing the catalytic domain, including structures in complex with known inhibitors, suggests that OGA is functional as a dimer and defines opportunities for structure-based drug design.

    • Nathaniel L Elsen
    • Sangita B Patel
    • Daniel J Klein
    Research
    Nature Chemical Biology
    Volume: 13, P: 613-615

  • 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

  • Human leukotriene B4 receptors (BLT1 and BLT2) are members of the GPCR superfamily that respond to a potent pro-inflammatory lipid and chemoattractant LTB4. Here authors determined a crystal structure of the human BLT1 in complex with a selective antagonist MK-D-046 and provide insights into hBLT1 ligand recognition and its mechanism of action.

    • Nairie Michaelian
    • Anastasiia Sadybekov
    • Vadim Cherezov
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-12

  • Various herpesvirus therapeutics target the viral DNA polymerase. Here, the authors present the crystal structure of herpesvirus polymerase in the elongating state with bound primer-template DNA and the broad-spectrum non-nucleoside inhibitor PNU-183792, which is of interest for further drug design.

    • Robert P. Hayes
    • Mee Ra Heo
    • Daniel Klein
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-7

  • Respiratory syncytial virus (RSV) is a leading cause of infant hospitalization. Here, the authors isolate a human monoclonal antibody that binds to a highly conserved epitope on the RSV fusion protein, neutralizes RSV A and B subtypes equipotently and is protective in the cotton rat model.

    • Aimin Tang
    • Zhifeng Chen
    • Kalpit A. Vora
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-13

  • Crystal structures of two complexes of the angiotensin II receptor AT2R with distinct tightly bound ligands reveal an active-like state of the receptor, in which helix VIII adopts a non-canonical position that blocks binding of G proteins and β-arrestins.

    • Haitao Zhang
    • Gye Won Han
    • Vadim Cherezov
    Research
    Nature
    Volume: 544, P: 327-332