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A list by Biophysics Colab

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  1. Mapping the molecular motions of 5-HT3 serotonin-gated channel by voltage-clamp fluorometry

    1. Laurie Peverini
    2. Sophie Shi
    3. Karima Medjebeur
    4. Pierre-Jean Corringer

    • Curated by eLife

      eLife assessment

      This valuable study applies voltage clamp fluorometry to provide new information about the function of serotonin-gated ion channels 5-HT3AR. The authors convincingly investigate structural changes inside and outside the orthosteric site elicited by agonists, partial agonists, and antagonists, helping to annotate existing cryo-EM structures. This work confirms that the activation of 5-HT3 receptors is similar to other members of this well-studied receptor superfamily. The work will be of interest to scientists working on channel biophysics but also drug development targeting ligand-gated ion channels.

    Reviewed by eLife

    9 evaluationsAppears in 2 listsLatest version Latest activity

  3. Structure-guided mutagenesis of OSCAs reveals differential activation to mechanical stimuli

    1. Sebastian Jojoa-Cruz
    2. Adrienne E Dubin
    3. Wen-Hsin Lee
    4. Andrew B Ward

    • Curated by eLife

      eLife assessment

      The manuscript seeks to dissect the molecular underpinnings of poke and stretch activation in OSCA channels. While the structural and functional experiments are well done, and the authors present some important data, the reviewers identified weaknesses in experimental design and interpretation that render the data incomplete in supporting some of the main conclusions of the paper. Nevertheless, this work will be of interest to those working in the fields of mechanosensation, sensory biology, and ion channels.

    Reviewed by eLife

    9 evaluationsAppears in 2 listsLatest version Latest activity

  4. MFSD7c functions as a transporter of choline at the blood–brain barrier

    1. Xuan Thi Anh Nguyen
    2. Thanh Nha Uyen Le
    3. Toan Q. Nguyen
    4. Hoa Thi Thuy Ha
    5. Anna Artati
    6. Nancy C. P. Leong
    7. Dat T. Nguyen
    8. Pei Yen Lim
    9. Adelia Vicanatalita Susanto
    10. Qianhui Huang
    11. Ling Fam
    12. Lo Ngah Leong
    13. Isabelle Bonne
    14. Angela Lee
    15. Jorge L. Granadillo
    16. Catherine Gooch
    17. Dejie Yu
    18. Hua Huang
    19. Tuck Wah Soong
    20. Matthew Wook Chang
    21. Markus R. Wenk
    22. Jerzy Adamski
    23. Amaury Cazenave-Gassiot
    24. Long N. Nguyen
    Appears in 1 listLatest version

  5. Characterization of binding kinetics and intracellular signaling of new psychoactive substances targeting cannabinoid receptor using transition-based reweighting method

    1. Soumajit Dutta
    2. Diwakar Shukla

    • Curated by eLife

      eLife Assessment

      A combination of molecular dynamics simulation and state-of-the-art statistical post-processing techniques provided valuable insight into GPCR-ligand dynamics. This manuscript provides solid evidence for differences in the binding/unbinding of classical cannabinoid drugs from new psychoactive substances. The results could aid in mitigating the public health threat these drugs pose.

    Reviewed by eLife

    7 evaluationsAppears in 2 listsLatest version Latest activity

  14. Mobile barrier mechanisms for Na+-coupled symport in an MFS sugar transporter

    1. Parameswaran Hariharan
    2. Yuqi Shi
    3. Satoshi Katsube
    4. Katleen Willibal
    5. Nathan D Burrows
    6. Patrick Mitchell
    7. Amirhossein Bakhtiiari
    8. Samantha Stanfield
    9. Els Pardon
    10. H Ronald Kaback
    11. Ruibin Liang
    12. Jan Steyaert
    13. Rosa Viner
    14. Lan Guan

    • Curated by eLife

      eLife assessment

      In an important study that will be of interest to the mechanistic membrane transport community, the authors capture the first cryo-EM structure of the inward facing melbiose transporter MelB, a well-studied model transporter from the major facilitator (MFS) superfamily. Cryo-EM experiments and supporting biophysical experiments provide solid evidence for transporter conformational changes.

    Reviewed by eLife

    9 evaluationsAppears in 2 listsLatest version Latest activity

  16. Discovery of a functionally selective serotonin 5-HT 1A receptor agonist for the treatment of pain

    1. Annika Ullrich
    2. Johannes Schneider
    3. JoĂŁo M. Braz
    4. Eduard Neu
    5. Nico Staffen
    6. Markus Stanek
    7. Jana Bláhová
    8. Tamsanqa Hove
    9. Tamara Albert
    10. Anni Allikalt
    11. Stefan Löber
    12. Karnika Bhardwaj
    13. Sian Rodriguez-Rosado
    14. Elissa Fink
    15. Tim Rasmussen
    16. Harald HĂĽbner
    17. Asuka Inoue
    18. Brian K. Shoichet
    19. Allan J. Basbaum
    20. Bettina Böttcher
    21. Dorothee Weikert
    22. Peter Gmeiner
    Appears in 1 listLatest version

  18. Structural insights into the orthosteric inhibition of P2X receptors by non-ATP analog antagonists

    1. Danqi Sheng
    2. Chen-Xi Yue
    3. Fei Jin
    4. Yao Wang
    5. Muneyoshi Ichikawa
    6. Ye Yu
    7. Chang-Run Guo
    8. Motoyuki Hattori

    • Curated by eLife

      eLife assessment

      This study by Sheng and colleagues provides valuable insights into the mechanism of competitive inhibitors of P2X receptors. The structural and functional evidence supporting the subtype specificity of pyridoxal-5'-phosphate derivatives is compelling and provides information for designing drugs that selectively target different subtypes of P2X receptor channels. The work will be of interest to biochemists, structural biologists, and pharmacologists.

    Reviewed by eLife

    7 evaluationsAppears in 2 listsLatest version Latest activity

  19. Conformational dynamics of a nicotinic receptor neurotransmitter site

    1. Mrityunjay Singh
    2. Dinesh C Indurthi
    3. Lovika Mittal
    4. Anthony Auerbach
    5. Shailendra Asthana

    • Curated by eLife

      eLife Assessment

      This useful work provides insight into agonist binding to nicotinic acetylcholine receptors, which is the stimulus for channel activation that regulates muscle contraction at the neuromuscular junction. The authors use in silico methods to explore the transient conformational change from a low to high affinity agonist-bound conformation as occurs during channel opening, but for which structural information is lacking owing to its transient nature. The simulations indicating that ligands flip ~180 degrees in the binding site as it transitions from a low to high affinity bound conformation are solid. A limitation is the approximation of binding energies using Poisson-Boltzmann Surface Area and mismatch between calculated and experimental binding energies for two of the four ligands tested. Nonetheless, this work presents an intriguing picture for the nature of a transient conformational change at the agonist binding site correlated with channel opening.

    Reviewed by eLife

    17 evaluationsAppears in 2 listsLatest version Latest activity
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