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Synthesis and Biochemical Evaluation of Monocarboxylic GRB2 SH2 Domain Inhibitors

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SH2 Domains

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2705))

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Abstract

This protocol discloses the synthesis of monocarboxylic inhibitors with a macrocyclic peptide scaffold to bind with the GRB2 SH2 domain and disrupt the protein–protein interactions (PPIs) between GRB2 and phosphotyrosine-containing proteins.

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Acknowledgments

This work was supported by 2017 and 2018 Moffitt Cancer Center Molecular Medicine (MM) Program Innovation Funds and 2019 Moffitt Cancer Center Lung Cancer Center for Excellence DeBartolo Thoracic Research Funds. We also thank the Moffitt Chemical Biology Core for use of the NMR and mass spectrometry facilities supported by National Cancer Institute grant P30-CA76292.

Author information

Authors and Affiliations

  1. Drug Discovery Department, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL, USA

    Tao **ao, Min Zhang & Haitao Ji

  2. Departments of Oncologic Sciences and Chemistry, University of South Florida, Tampa, FL, USA

    Tao **ao, Min Zhang & Haitao Ji

Authors
  1. Tao **ao
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  2. Min Zhang
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  3. Haitao Ji
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Corresponding author

Correspondence to Haitao Ji .

Editor information

Editors and Affiliations

  1. School of Biosciences, College of Life and Environmental Sciences, University of Birmingham, Birmingham, UK

    Teresa Carlomagno

  2. Signalling Research Centres BIOSS &CIBSS, University of Freiburg, Freiburg, Germany

    Maja Köhn

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© 2023 The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature

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**ao, T., Zhang, M., Ji, H. (2023). Synthesis and Biochemical Evaluation of Monocarboxylic GRB2 SH2 Domain Inhibitors. In: Carlomagno, T., Köhn, M. (eds) SH2 Domains. Methods in Molecular Biology, vol 2705. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-3393-9_15

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  • DOI: https://doi.org/10.1007/978-1-0716-3393-9_15

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  • Publisher Name: Humana, New York, NY

  • Print ISBN: 978-1-0716-3392-2

  • Online ISBN: 978-1-0716-3393-9

  • eBook Packages: Springer Protocols

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