Overview of Chemical Diversity

David J. Triggle1

1 The State University of New York, Buffalo, New York
Publication Name:  Current Protocols in Pharmacology
Unit Number:  Unit 9.1
DOI:  10.1002/0471141755.ph0901s10
Online Posting Date:  May, 2001
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In the search for new compounds and the identification of compound sources by the pharmaceutical industry, natural products continue to play an extremely important role, principally because they represent a source, real and potential, of remarkable molecular diversity. Although advances in drug discovery have been significantly fueled and paralleled by advances in synthetic organic chemistry, structural biology, and computational chemistry, they continue to be linked to both natural product and biological chemistry. The dramatic progress in synthetic molecular diversity achieved through combinatorial chemistry is heavily influenced by our understanding of biologically driven molecular diversity. Additionally, through advances in genomics, synthetic chemistry is being linked to biochemical systems to create hybrid “natural‐synthetic“ products, “unnatural“ peptides and “self‐evolving“ molecules. This unit discusses specific instances where diversity is generated by exploitation of biological pathways. These strategies are intimately linked to processes of biological screening, and in particular to high‐throughput screening.

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Table of Contents

  • High‐Throughput Screening (HTS)
  • Natural Products and the Screening of Biodiversity
  • Modification of Existing Structures
  • Rationally Planned Approaches
  • Identification and Exploitation of Basic Pharmacophores
  • Combinational Chemistry
  • Evolutionary Chemistry
  • Orphan Ligands and Orphan Receptors
  • Literature Cited
  • Figures
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Literature Cited

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