Contents

Abstract 15

3.1 Introduction 16

3.2 GPCR Family Overview 16

3.3 GPCR Tractability: Current Therapeutics 19

3.4 GPCR Drug Discovery 22

3.4.1 GPCR Target Discovery and Selection 22

3.4.1.1 Bioinformatics Approaches for GPCR Discovery 22

3.4.1.2 GPCR Localization 23

3.4.1.3 GPCR Target Validation 24

3.4.1.4 GPCR Draggability 27

3.4.2 Lead Optimization 28

3.5 Novel GPCR Features and Impact on Drug Discovery Approaches 29

3.5.1 Orphan GPCRs 30

3.5.2 GPCR Oligomerization 30

3.6 Summary 32

References 32

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