Evidence map›Paper›PMID 31709066›Full record

ArticleIUCrJ2019

Toward G protein-coupled receptor structure-based drug design using X-ray lasers.

Andrii Ishchenko, Benjamin Stauch, Gye Won Han, Alexander Batyuk, Anna Shiriaeva, Chufeng Li, Nadia Zatsepin, Uwe Weierstall, Wei Liu, Eriko Nango and 8 more

Abstract read
In one paragraph

Article in IUCrJ, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.

0numbers the graph read from it
0cells of the map it votes in
41citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

41 citing papers in PubMed.

  1. Article
  2. A novel fusion tool to enable G protein-coupled receptor structure determination.Acta crystallographica. Section D, Structural biology · 2026
    Article
  3. Article
  4. Article
  5. Structural Mechanism of an Efficacy Photoswitch Targeting the βAngewandte Chemie (International ed. in English) · 2026
    Article
  6. Article
  7. Investigating the electrostatics underlying activation of the βBiochimica et biophysica acta. Biomembranes · 2026
    Article
  8. Review
  9. Structural insights into nonpeptide antagonist inhibition of somatostatin receptor subtype 5.Proceedings of the National Academy of Sciences of the United States of America · 2025
    Article
  10. Review
  11. Review
  12. G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024
    Article
  13. Melatonin and Related Compounds as Antioxidants.Mini reviews in medicinal chemistry · 2024
    Review
  14. Article
  15. Article
  16. Article
  17. A Novel "Activation Switch" Motif Common to All Aminergic Receptors.Journal of chemical information and modeling · 2023
    Review
  18. MicroED in drug discovery.Current opinion in structural biology · 2023
    Review
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

18 authors.

Andrii IshchenkoBridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA.
Benjamin StauchBridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA.ORCID https://orcid.org/0000-0001-7626-2021
Gye Won HanBridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA.
Alexander BatyukLinac Coherent Light Source, SLAC National Accelerator Laboratory, Menlo Park, CA 94025, USA.
Anna ShiriaevaBridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA.
Chufeng LiDepartment of Physics, Arizona State University, Tempe, AZ 85287, USA.ORCID https://orcid.org/0000-0002-2997-0903
Nadia ZatsepinDepartment of Physics, Arizona State University, Tempe, AZ 85287, USA.ORCID https://orcid.org/0000-0003-1757-0205
Uwe WeierstallDepartment of Physics, Arizona State University, Tempe, AZ 85287, USA.
Wei LiuSchool of Molecular Sciences and Biodesign Center for Applied Structural Discovery, Biodesign Institute, Arizona State University, Tempe, AZ 85287, USA.
Eriko NangoRIKEN SPring-8 Center, 1-1-1 Kouto, Sayo-cho, Sayo-gun, Hyogo 679-5148, Japan.
Takanori NakaneDepartment of Biological Sciences, Graduate School of Science, The University of Tokyo, 2-11-16 Yayoi, Bunkyo, Tokyo 113-0032, Japan.ORCID https://orcid.org/0000-0003-2697-2767
Rie TanakaRIKEN SPring-8 Center, 1-1-1 Kouto, Sayo-cho, Sayo-gun, Hyogo 679-5148, Japan.ORCID https://orcid.org/0000-0003-1062-4792
Kensuke TonoJapan Synchrotron Radiation Research Institute, 1-1-1 Kouto, Sayo-cho, Sayo-gun, Hyogo 679-5198, Japan.ORCID https://orcid.org/0000-0003-1218-3759
Yasumasa JotiJapan Synchrotron Radiation Research Institute, 1-1-1 Kouto, Sayo-cho, Sayo-gun, Hyogo 679-5198, Japan.ORCID https://orcid.org/0000-0002-4040-5972
So IwataRIKEN SPring-8 Center, 1-1-1 Kouto, Sayo-cho, Sayo-gun, Hyogo 679-5148, Japan.
Isabel MoraesNational Physical Laboratory, Hampton Road, Teddington TW11 0LW, England.
Cornelius GatiDepartment of Structural Biology, Stanford University, Stanford, CA 94305, USA.
Vadim CherezovBridge Institute, Departments of Chemistry and Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA.ORCID https://orcid.org/0000-0002-5265-3914

Funding

Structural Biology Of G Protein-Coupled ReceptorsR35GM127086 · NIGMS · UNIVERSITY OF SOUTHERN CALIFORNIA · PI Vadim Cherezov · 2018 to 2026
$3.6M
Structure Determination of G Protein-Coupled Receptors by Microcrystal Electron DiffractionR01GM124152 · NIGMS · ARIZONA STATE UNIVERSITY-TEMPE CAMPUS · PI NANNENGA, BRENT · 2017 to 2021
$1.6M
Structure and Function of Dopamine ReceptorsR21DA042298 · NIDA · ARIZONA STATE UNIVERSITY-TEMPE CAMPUS · PI LIU, WEI · 2017 to 2018
$404k
NIDA NIH HHS R21 DA042298NIGMS NIH HHS R01 GM124152NIGMS NIH HHS R35 GM127086Wellcome Trust
6 · The paper itself

Abstract

Rational structure-based drug design (SBDD) relies on the availability of a large number of co-crystal structures to map the ligand-binding pocket of the target protein and use this information for lead-compound optimization via an iterative process. While SBDD has proven successful for many drug-discovery projects, its application to G protein-coupled receptors (GPCRs) has been limited owing to extreme difficulties with their crystallization. Here, a method is presented for the rapid determination of multiple co-crystal structures for a target GPCR in complex with various ligands, taking advantage of the serial femtosecond crystallography approach, which obviates the need for large crystals and requires only submilligram quantities of purified protein. The method was applied to the human β

Indexed as

drug discoveryG protein-coupled receptorsmembrane proteinsmolecular recognitionprotein structureserial femtosecond crystallographystructure determinationX-ray free-electron lasers

Identifiers

PMID31709066
PMCPMC6830214

What OpenQuestion holds

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LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.