Contents

4.1 Introduction 59

4.2 Small Molecules 60

4.2.1 Generation of Small-Molecule Probes 60

4.2.1. 1 Diversity-Oriented Synthesis 61

4.2.1.2 Fragment-Based Approaches 62

4.2.2 Applying Small Molecules in Biology 63

4.2.2.1 Chemical Genetics 64

4.2.2.2 ChemBank and PubChem 65

4.3 Modifying Biomacromolecules 65

4.3.1 Protein Engineering 66

4.3.2 Unnatural Mutagenesis 68

4.3.3 Peptide/Protein Ligation 71

4.3.4 Chemical Modification of Proteins 72

4.4 Concluding Remarks 73

Further Readings 74

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