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Open Access
Peer-reviewed
Research Article
Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM
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Frances M. Bashore ,
Contributed equally to this work with: Frances M. Bashore, Vittorio L. Katis, Yuhong Du
Roles Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Visualization, Writing – original draft, Writing – review & editing
Affiliation Structural Genomics Consortium, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America
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Vittorio L. Katis ,
Contributed equally to this work with: Frances M. Bashore, Vittorio L. Katis, Yuhong Du
Roles Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Visualization, Writing – review & editing
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Yuhong Du ,
Contributed equally to this work with: Frances M. Bashore, Vittorio L. Katis, Yuhong Du
Roles Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Visualization, Writing – review & editing
Affiliations Department of Pharmacology and Chemical Biology, School of Medicine, Emory University, Atlanta, GA, United States of America, Emory Chemical Biology Discovery Center, School of Medicine, Emory University, Atlanta, GA, United States of America
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Arunima Sikdar,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Division of Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America
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Dongxue Wang,
Roles Data curation, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliations Department of Pharmacology and Chemical Biology, School of Medicine, Emory University, Atlanta, GA, United States of America, Emory Chemical Biology Discovery Center, School of Medicine, Emory University, Atlanta, GA, United States of America
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William J. Bradshaw,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Karolina A. Rygiel,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Tina M. Leisner,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Division of Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America
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Rod Chalk,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Swati Mishra,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliations Department of Laboratory Medicine and Pathology, School of Medicine, University of Washington, Seattle, WA, United States of America, Institute for Stem Cell and Regenerative Medicine, School of Medicine, University of Washington, Seattle, WA, United States of America
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C. Andrew Williams,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliations Department of Laboratory Medicine and Pathology, School of Medicine, University of Washington, Seattle, WA, United States of America, Institute for Stem Cell and Regenerative Medicine, School of Medicine, University of Washington, Seattle, WA, United States of America
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Opher Gileadi,
Roles Conceptualization, Funding acquisition, Supervision, Writing – review & editing
Current address: Structural Genomics Consortium, Department of Medicine, Karolinska Hospital and Karolinska Institute, Stockholm, Sweden
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Paul E. Brennan,
Roles Conceptualization, Funding acquisition, Supervision, Writing – review & editing
Affiliation Nuffield Department of Medicine, Centre for Medicines Discovery, ARUK Oxford Drug Discovery Institute, University of Oxford, Headington, Oxford, United Kingdom
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Jesse C. Wiley,
Roles Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Resources, Supervision, Validation, Visualization, Writing – review & editing
Affiliation Sage Bionetworks, Seattle, WA, United States of America
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Jake Gockley,
Roles Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Writing – review & editing
Affiliation Sage Bionetworks, Seattle, WA, United States of America
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Gregory A. Cary,
Roles Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Resources, Validation, Visualization, Writing – review & editing
Affiliation The Jackson Laboratory for Mammalian Genetics, Bar Harbor, ME, United States of America
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Gregory W. Carter,
Roles Conceptualization, Funding acquisition, Supervision, Writing – review & editing
Affiliation The Jackson Laboratory for Mammalian Genetics, Bar Harbor, ME, United States of America
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Jessica E. Young,
Roles Conceptualization, Supervision, Writing – review & editing
Affiliations Department of Laboratory Medicine and Pathology, School of Medicine, University of Washington, Seattle, WA, United States of America, Institute for Stem Cell and Regenerative Medicine, School of Medicine, University of Washington, Seattle, WA, United States of America
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Kenneth H. Pearce,
Roles Conceptualization, Supervision, Writing – review & editing
Affiliation Division of Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America
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Haian Fu,
Roles Conceptualization, Funding acquisition, Supervision, Writing – review & editing
Affiliations Department of Pharmacology and Chemical Biology, School of Medicine, Emory University, Atlanta, GA, United States of America, Emory Chemical Biology Discovery Center, School of Medicine, Emory University, Atlanta, GA, United States of America
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the Emory-Sage-SGC TREAT-AD Center ,
¶Members of the Emory-Sage-SGC TREAT-AD Center are provided in the Acknowledgments Section.
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Alison D. Axtman
Roles Conceptualization, Funding acquisition, Project administration, Supervision, Writing – review & editing
* E-mail: alison.axtman@unc.edu
Affiliation Structural Genomics Consortium, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, United States of America
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Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM
- Frances M. Bashore,
- Vittorio L. Katis,
- Yuhong Du,
- Arunima Sikdar,
- Dongxue Wang,
- William J. Bradshaw,
- Karolina A. Rygiel,
- Tina M. Leisner,
- Rod Chalk,
- Swati Mishra
- Published: February 15, 2024
- https://doi.org/10.1371/journal.pone.0293548
- See the preprint