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Showing 1–10 of 10 results
Advanced filters: Author: Kuglae Kim Clear advanced filters
  • Glutamine addiction is a hallmark of many cancers. iMQT_020, a first-in-class allosteric inhibitor of the mitochondrial glutamine transporter SLC1A5_var, disrupts glutamine-dependent mitochondrial metabolism, selectively killing cancer cells and enhancing immune checkpoint inhibitor efficacy.

    • Yulseung Sung
    • Ya Chun Yu
    • Jung Min Han
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-25
  • Biased signaling in κ-opiod receptors (KOR) offer an attractive strategy for pain management. Here the authors identify determinants of KOR signaling bias using structural methods in combination with molecular dynamics simulations.

    • Amal El Daibani
    • Joseph M. Paggi
    • Tao Che
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-13
  • The authors present 7 cryo-EM structures of hallucinogenic and non-hallucinogenic compounds across multiple chemotypes bound to the 5-HT2A receptor, shedding light onto ligand specificity and signaling bias.

    • Ryan H. Gumpper
    • Manish K. Jain
    • Bryan L. Roth
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-13
  • Using cryo-EM, authors reveal the structure and activation mechanism of GPR156, a class C orphan GPCR implicated in sound detection. They find that GPR156 is a transducer for phospholipid signaling and provide insights into the basis for its constitutive activation.

    • Jinwoo Shin
    • Junhyeon Park
    • Yunje Cho
    Research
    Nature Structural & Molecular Biology
    Volume: 31, P: 678-687
  • Structural studies of the itch receptors MRGPRX2 and MRGPRX4 in complex with endogenous and synthetic ligands provide a basis for the development of therapeutic compounds for pain, itch and mast cell-mediated hypersensitivity.

    • Can Cao
    • Hye Jin Kang
    • Bryan L. Roth
    Research
    Nature
    Volume: 600, P: 170-175
  • This comprehensive study of the most enigmatic serotonin receptor 5-HT5AR includes lots of pharmacological investigations, inactive and active state structures with antagonist, partial agonist and full agonists. Also, a highly potent and selective antagonist was developed.

    • Shicheng Zhang
    • He Chen
    • Bryan L. Roth
    Research
    Nature Structural & Molecular Biology
    Volume: 29, P: 677-687
  • Recent studies revealed that G protein-coupled receptors rapidly interconvert between multiple states. Here, authors use the kappa opioid receptor (KOR) and show how two state-dependent nanobodies provide real-time reporting of ligand stabilized states with KOR and other GPCRs.

    • Tao Che
    • Justin English
    • Bryan L. Roth
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-12