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Fragment-Based Drug Design

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Book cover Chemical Library Design

Part of the book series: Methods in Molecular Biology ((MIMB,volume 685))

Abstract

Fragment-based drug design (FBDD), which is comprised of both fragment screening and the use of fragment hits to design leads, began more than 15 years ago and has been steadily gaining in popularity and utility. Its origin lies on the fact that the coverage of chemical space and the binding efficiency of hits are directly related to the size of the compounds screened. Nevertheless, FBDD still faces challenges, among them developing fragment screening libraries that ensure optimal coverage of chemical space, physical properties and chemical tractability. Fragment screening also requires sensitive assays, often biophysical in nature, to detect weak binders. In this chapter we will introduce the technologies used to address these challenges and outline the experimental advantages that make FBDD one of the most popular new hit-to-lead process.

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Author information

Authors and Affiliations

  1. Pfizer Global R&D, Cambridge, MA, USA

    Eric Feyfant, Kevin Paris & Désirée H.H. Tsao

  2. Cubist pharmaceuticals, Inc., Lexington, MA, USA

    Jason B. Cross

Authors
  1. Eric Feyfant
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  2. Jason B. Cross
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  3. Kevin Paris
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  4. Désirée H.H. Tsao
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Editor information

Editors and Affiliations

  1. , Department of Pharmacology, University of California, La Jolla, 92093, California, USA

    Joe Zhongxiang Zhou

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Feyfant, E., Cross, J.B., Paris, K., Tsao, D.H. (2011). Fragment-Based Drug Design. In: Zhou, J. (eds) Chemical Library Design. Methods in Molecular Biology, vol 685. Humana Press. https://doi.org/10.1007/978-1-60761-931-4_12

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  • DOI: https://doi.org/10.1007/978-1-60761-931-4_12

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  • Publisher Name: Humana Press

  • Print ISBN: 978-1-60761-930-7

  • Online ISBN: 978-1-60761-931-4

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