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Next Generation Kinase Inhibitors

Moving Beyond the ATP Binding/Catalytic Sites

  • Book
  • © 2020

Overview

Editors:
  1. Paul Shapiro

    1. Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, USA

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  • This book provides a brief review of drug development efforts and FDA approved kinase inhibitors

  • This book sets the stage and highlights the importance of kinase signaling pathways in physiological processes

  • This book identifies the genetic mutations that lead to kinase dysregulation and how this promotes the growth and survival of cancer cells

  • The book discusses the emergence of resistance to kinase inhibitors

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Table of contents (8 chapters)

  1. Front Matter

    Pages i-xii
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  2. Introduction to Kinases, Cellular Signaling, and Kinase Inhibitors

    • Paul Shapiro, Ramon Martinez III, Amy Defnet
    Pages 1-12

  3. Overview of Current Type I/II Kinase Inhibitors

    • Zheng Zhao, Philip E. Bourne
    Pages 13-28

  4. Avoiding or Co-Opting ATP Inhibition: Overview of Type III, IV, V, and VI Kinase Inhibitors

    • Ramon Martinez III, Amy Defnet, Paul Shapiro
    Pages 29-59

  5. Protein Kinase Interactions with Regulatory and Effector Proteins

    • Amy Defnet, Ramon Martinez III, Paul Shapiro
    Pages 61-80

  6. Developing Kinase Inhibitors Using Computer-Aided Drug Design Approaches

    • Wenbo Yu, David J. Weber, Paul Shapiro, Alexander D. MacKerell Jr
    Pages 81-108

  7. A Toolbox of Structural Biology and Enzyme Kinetics Reveals the Case for ERK Docking Site Inhibition

    • Rachel M. Sammons, Kevin N. Dalby
    Pages 109-139

  8. Novel Stabilized Peptide Inhibitors of Protein Kinases

    • Leah G. Helton, Ameya J. Limaye, George N. Bendzunas, Eileen J. Kennedy
    Pages 141-167

  9. Novel Peptide-Based Inhibitors of Protein Kinases

    • Justin M. Holub
    Pages 169-206

  10. Back Matter

    Pages 207-217
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Keywords

About this book

Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease. 

Editors and Affiliations

  • Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, USA

    Paul Shapiro

About the editor

Paul Shapiro has a long-standing interest in protein kinases and their role in regulating cellular functions during disease. Specific areas focus on the discovery and development of function-selective mitogen-activated protein (MAP) kinase inhibitors with the goal of mitigating cancer cell proliferation and inflammation-induced lung injury associated with respiratory diseases. He received a Bachelor of Science degree from the University of Wisconsin-Madison and his doctorate in molecular physiology and biophysics from the University of Vermont. Dr. Shapiro completed post-doctoral training in the Department of Chemistry and Biochemistry at the University of Colorado-Boulder and is currently a professor of Pharmaceutical Sciences at the University of Maryland School of Pharmacy.

Bibliographic Information

  • Book Title: Next Generation Kinase Inhibitors

  • Book Subtitle: Moving Beyond the ATP Binding/Catalytic Sites

  • Editors: Paul Shapiro

  • DOI: https://doi.org/10.1007/978-3-030-48283-1

  • Publisher: Springer Cham

  • eBook Packages: Biomedical and Life Sciences, Biomedical and Life Sciences (R0)

  • Copyright Information: Springer Nature Switzerland AG 2020

  • Hardcover ISBN: 978-3-030-48282-4Published: 15 July 2020

  • Softcover ISBN: 978-3-030-48285-5Published: 15 July 2021

  • eBook ISBN: 978-3-030-48283-1Published: 14 July 2020

  • Edition Number: 1

  • Number of Pages: XII, 217

  • Number of Illustrations: 3 b/w illustrations, 56 illustrations in colour

  • Topics: Cancer Research

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