Cited by 136Click Chemistry and ApplicationsChemical Synthesis and AnalysisProtein Degradation and Inhibitors

Fragment-based covalent ligand discovery

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Lu, Wenchao, Kostic, Milka, Zhang, Tinghu, Che, Jianwei, Patricelli, Matthew P., Jones, Lyn H., Chouchani, Edward T., Gray, Nathanael S.·2021·RSC Chemical Biology

Abstract

Covalent fragment-based ligand discovery greatly facilitates the discovery of useful fragments for drug discovery and helps unveil chemical-tractable biological targets in native biological systems.

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Crossref · 10.1039/d0cb00222d

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  • Covalent ligand screening from electrophilic compound libraries is becoming more common.

    “Covalent ligand screening is another ligand discovery approach that is becoming more common, whereby various methods are used to discover covalent ligands from libraries of electrophilic compounds7,12,13.”

    From Advances in covalent drug discovery (2022) · cites this paper as [13]

  • Over the past decade, covalent ligand discovery has shifted towards screening more drug-like electrophilic fragments.

    “Over the past decade, covalent ligand discovery has shifted towards screening more drug-like electrophilic fragments13.”

    From Advances in covalent drug discovery (2022) · cites this paper as [13]

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References 121 · Cited by 136

Research works printed but not linked: 7

  1. Strelow J. M. SLAS Discovery 2017 22 3 20 27703080
  2. Xiao H. Jedrychowski M. P. Schweppe D. K. Huttlin E. L. Yu Q. Heppner D. E. Li J. Long J. Mills E. L. Szpyt J. He Z. Du G. Garrity R. Reddy A. Vaites L. P. Paulo J. A. Zhang T. Gray N. S. Gygi S. P. Chouchani E. T. Cell 2020 180 968-983 e924 PMC8164166 32109415
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  7. Tang B. He F. Liu D. Fang M. Wu Z. Xu D. bioRxiv 2020 10.1101/2020.03.03.972133 · DOI

Authors
Lu, W., Kostic, M., Zhang, T., Che, J., Patricelli, M. P., Jones, L. H., Chouchani, E. T., & Gray, N. S.
Affiliations
  • Harvard University (US)
  • Department of Cancer Biology
  • Vividion Therapeutics (United States) (US)
  • Dana-Farber Cancer Institute (US)
Corresponding author
Gray, Nathanael S.
Venue
RSC Chemical Biology
Published
2021
Volume
2
Issue
2
Pages
354-367
ISSN
2633-0679 (ISSN-L)
OpenAlex
W3128963846
Cited by
136
References
121
Citations by year
2026: 27 · 2025: 21 · 2024: 23 · 2023: 34 · 2022: 24 · 2021: 7
FWCI
1.81
Type
journal article
Language
en
Open access
Locations
  • RSC Chemical Biology (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
Topics
  • Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Keywords
targeted covalent inhibitors, chemoproteomics, undruggable proteins, proteome-wide screening

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