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Showing 1–12 of 12 results
Advanced filters: Author: Susruta Majumdar Clear advanced filters

  • 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

  • Ibogaine is a natural substance that interrupts opioid addiction but has cardiac risks. This article introduces novel ibogaine analogs that show reduced cardiac risk and enhanced neuroplasticity and therapeutic-like effects in models of opioid use disorder.

    • Václav Havel
    • Andrew C. Kruegel
    • Dalibor Sames
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-21

  • δ-Opioid receptors (δOR) are promising targets for pain management with reduced side effects. Here, the authors use a structure-based approach to design and characterize C6-Quino, a selective δOR partial agonist, highlighting its potential therapeutic relevance.

    • Balazs R. Varga
    • Sarah M. Bernhard
    • Tao Che
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-15

  • Compounds have been made that activate only the G-protein signalling pathway when bound to the µ-opioid receptor — the target of opioid pain relievers. These compounds lack one of the main side effects of currently used opioids.

    • Susruta Majumdar
    • Lakshmi A. Devi
    News & Views
    Nature
    Volume: 553, P: 286-288

  • Despite advances in GPCR structures and peptide design, creating high-affinity ligands remains a challenge. Here the authors develop a computational method, successfully identifying peptide-based molecules for KOR: their platform shows promise for streamlined GPCR ligand discovery.

    • Edin Muratspahić
    • Kristine Deibler
    • Christian W. Gruber
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-17

  • 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

  • Bitopic functionalized ligands based on fentanyl can target the sodium ion-binding site of the mu-opioid receptor and selectively modulate downstream signalling pathways, potentially leading to safer analgesics.

    • Abdelfattah Faouzi
    • Haoqing Wang
    • Susruta Majumdar
    Research
    Nature
    Volume: 613, P: 767-774

  • Mitragynine (MG) is an indole alkaloid from kratom plant that binds opioid receptors and as such presents a scaffold for the development of atypical opioid receptor modulators. Here, the authors report a synthetic method for selective functionalization of the C11 position of MG, and show that this position is essential for fine-tuning opioid receptor signaling efficacy.

    • Srijita Bhowmik
    • Juraj Galeta
    • Dalibor Sames
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-14

  • Active-state structures of the κ-opioid receptor in complexes with the G-protein heterotrimers Gi1, GoA, Gz and Gg provide insights into the actions of hallucinogenic opioids and G-protein-coupling specificity at the κ-opioid receptor.

    • Jianming Han
    • Jingying Zhang
    • Tao Che
    ResearchOpen Access
    Nature
    Volume: 617, P: 417-425

  • Cryo-EM structures of µ-opioid receptor complexes with two agonists coupled to molecular dynamics simulations and functional assays highlight distinct efficacy for G protein subtype activation and β-arrestin recruitment.

    • Qianhui Qu
    • Weijiao Huang
    • Georgios Skiniotis
    Research
    Nature Chemical Biology
    Volume: 19, P: 423-430