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Target Identification, Lead Discovery, and Optimization

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Radiopharmaceutical Chemistry

Abstract

The selection of an appropriate target can make or break a radiopharmaceutical development program. Understanding the characteristics of a good target and creating ligands with high affinity, specificity, and ideal pharmacokinetics will lead to the creation of radiopharmaceuticals that will be invaluable to patient outcomes. In this chapter, we will introduce the notion of targeting, define the characteristics of the ideal target, and describe the most common ways used to identify and develop ligands specific to the target.

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Author information

Authors and Affiliations

  1. Department of Biomedical Engineering, School of Medicine, University of Virginia, Charlottesville, VA, USA

    Julien Dimastromatteo & Kimberly A. Kelly

Authors
  1. Julien Dimastromatteo
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  2. Kimberly A. Kelly
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Corresponding author

Correspondence to Kimberly A. Kelly .

Editor information

Editors and Affiliations

  1. Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, USA

    Jason S. Lewis

  2. Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands

    Albert D. Windhorst

  3. Department of Chemistry, Hunter College, City University of New York, New York, NY, USA

    Brian M. Zeglis

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Dimastromatteo, J., Kelly, K.A. (2019). Target Identification, Lead Discovery, and Optimization. In: Lewis, J., Windhorst, A., Zeglis, B. (eds) Radiopharmaceutical Chemistry. Springer, Cham. https://doi.org/10.1007/978-3-319-98947-1_32

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  • DOI: https://doi.org/10.1007/978-3-319-98947-1_32

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-98946-4

  • Online ISBN: 978-3-319-98947-1

  • eBook Packages: MedicineMedicine (R0)

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