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Showing 1–10 of 10 results
Advanced filters: Author: Yuki Shiimura Clear advanced filters

  • This study reveals how anamorelin, a superagonist targeting the ghrelin receptor, works compared to other drugs. Structural insights into ligand binding and genetic variations offer a framework for personalized therapies

    • Yuki Shiimura
    • Dohyun Im
    • Ikuo Masuho
    Research
    Nature Structural & Molecular Biology
    Volume: 32, P: 531-542

  • VMAT2 regulates neurotransmitter uptake into synaptic vesicles. Here, the authors determined the cryo-EM structures of VMAT2, providing a structural basis for understanding VMAT2- mediated vesicular transport of neurotransmitters.

    • Dohyun Im
    • Mika Jormakka
    • So Iwata
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-10

  • Histamine receptor H4R is implicated in chronic inflammatory diseases, such as asthma, arthritis, and atopic dermatitis. Here, the authors determined the first cryo-EM structure of the histamine H4 receptor, providing valuable structural insights for the design of drugs targeting H4R in chronic inflammatory diseases.

    • Dohyun Im
    • Jun-ichi Kishikawa
    • So Iwata
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-11

  • A peripherally restricted CB1 agonist (VIP36) targeting a cryptic receptor pocket was developed, showing high efficacy in mouse pain models with minimal side effects and tolerance, potentially revolutionizing chronic pain treatment and GPCR drug design.

    • Vipin Ashok Rangari
    • Evan S. O’Brien
    • Susruta Majumdar
    Research
    Nature
    Volume: 640, P: 265-273

  • Tummino et al. dock 74 million molecules against the human cannabinoid-1 receptor to find uM ligands. Optimization led to a nM agonist conferring analgesia with reduced side effects in mice, highlighting its potential as a pain therapeutic and the promise of a structure-based approach.

    • Tia A. Tummino
    • Christos Iliopoulos-Tsoutsouvas
    • Brian K. Shoichet
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-19

  • A newly discovered negative allosteric modulator of the µ-opioid receptor works together with naloxone to potently block opioid agonist signalling with reduced adverse effects.

    • Evan S. O’Brien
    • Vipin Ashok Rangari
    • Brian K. Kobilka
    Research
    Nature
    Volume: 631, P: 686-693

  • The dopamine D2 receptor (D2R) is a GPCR and an important drug target for schizophrenia treatment. Here, the authors present the crystal structure of human D2R in complex with the antipsychotic drug spiperone, which is of interest for designing antipsychotics with improved receptor selectivity.

    • Dohyun Im
    • Asuka Inoue
    • Tatsuro Shimamura
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-11

  • Ghrelin is a gastric peptide hormone with important physiological functions, including growth hormone release and appetite-stimulating activity. Here, authors solved the crystal structure of the ghrelin receptor bound to antagonist and suggested a possible mechanism of activation by acyl-modified ghrelin.

    • Yuki Shiimura
    • Shoichiro Horita
    • Masayasu Kojima
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-9

  • The crystal structure of human AT2R binding an angiotensin II analog reveals ‘core’ and ‘extended’ domains within the binding pocket. A signature positively charged motif orients the C terminus of the peptide ligand at the bottom of the binding pocket.

    • Hidetsugu Asada
    • Shoichiro Horita
    • So Iwata
    Research
    Nature Structural & Molecular Biology
    Volume: 25, P: 570-576