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Showing 1–16 of 16 results
Advanced filters: Author: Alisa Glukhova Clear advanced filters

  • The A3 adenosine receptor is a promising drug target for cancer, inflammation, and glaucoma. Here, authors determine atomic structures of the human A3 receptor, identifying a previously hidden binding pocket that will aid in the development of more effective A3 receptor-targeted medicines.

    • Liudi Zhang
    • Jesse I. Mobbs
    • David M. Thal
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-19

  • Lysosomal phospholipase A2 (LPLA2) and lecithin:cholesterol acyltransferase (LCAT) are important lipid metabolizing enzymes. Here the authors present crystal structures of LPLA2 and LCAT that reveal the unique architecture of this small family of enzymes involved in human physiology and disease.

    • Alisa Glukhova
    • Vania Hinkovska-Galcheva
    • John J. G. Tesmer
    Research
    Nature Communications
    Volume: 6, P: 1-12

  • The cryo-electron microscopy structure of the human adenosine A1 receptor in complex with adenosine and heterotrimeric Gi2 protein provides molecular insights into receptor and G-protein selectivity.

    • Christopher J. Draper-Joyce
    • Maryam Khoshouei
    • Arthur Christopoulos
    Research
    Nature
    Volume: 558, P: 559-563

  • Porcupine (PORCN) is an endoplasmic reticulum-resident membrane-bound O-acyltransferase that plays a crucial role in Wnt signalling and is as a therapeutic target for Wnt-driven cancers. Here, the authors use cryo-electron microscopy to elucidate the structures of human PORCN with inhibitors, uncovering key interactions mediating inhibitor binding and catalysis.

    • Katrina A. Black
    • Jesse I. Mobbs
    • Alisa Glukhova
    ResearchOpen Access
    Communications Chemistry
    Volume: 8, P: 1-9

  • MIPS521, a positive allosteric modulator of the adenosine A1 receptor, has analgesic properties in a rat model of neuropathic pain through a mechanism by which MIPS521 stabilizes the complex between adenosine, receptor and G protein.

    • Christopher J. Draper-Joyce
    • Rebecca Bhola
    • Arthur Christopoulos
    Research
    Nature
    Volume: 597, P: 571-576

  • The P2X1 receptor is a promising target for the development of a non-hormonal male contraceptive. Here, researchers determined the atomic structure of the P2X1 receptor, revealing opportunities for developing drugs to target this receptor.

    • Felix M. Bennetts
    • Hariprasad Venugopal
    • David M. Thal
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-14

  • The drug Xanomeline is progressing through clinical trials for the treatment of patients with schizophrenia. Here, the authors determine a cryo-EM structure of Xanomeline bound to its primary target revealing a dual binding mode mechanism.

    • Wessel A. C. Burger
    • Vi Pham
    • David M. Thal
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-11

  • The glucagon-like peptide-1 receptor (GLP-1R) can be targeted in the treatment of diabetes, obesity and other metabolic disorders. Here, the authors assess the molecular mechanisms of peptide agonists binding to GLP-1R and the responses elucidated by these ligands, including distinct kinetics of G protein activation.

    • Giuseppe Deganutti
    • Yi-Lynn Liang
    • Denise Wootten
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-18

  • The structure of a complex containing calcitonin gene-related peptide, the human calcitonin gene-related peptide receptor and the Gs heterotrimer, determined using Volta phase-plate cryo-electron microscopy, provides structural insight into the regulation of G-protein-coupled receptors by receptor activity modifying protein 1.

    • Yi-Lynn Liang
    • Maryam Khoshouei
    • Patrick M. Sexton
    Research
    Nature
    Volume: 561, P: 492-497

  • Unphosphorylated PINK1 of Pediculus humanus corporis forms a dimerized state before undergoing trans-autophosphorylation, and phosphorylated PINK1 undergoes a conformational change in the N-lobe to produce its phosphorylated, ubiquitin-binding state.

    • Zhong Yan Gan
    • Sylvie Callegari
    • David Komander
    Research
    Nature
    Volume: 602, P: 328-335

  • The class B secretin GPCR (SecR) has broad physiological effects, with target potential for treatment of metabolic and cardiovascular disease. Here, authors present a cryo-EM structure and biochemical studies of secretin binding to the SecR:Gs complex which show that interactions between peptide and receptor were dynamic.

    • Maoqing Dong
    • Giuseppe Deganutti
    • Laurence J. Miller
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-17