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GPCRs in Drug Discovery - Efforts to De-Orphanize Novel GPCR Targets are Increasing
Date:10/25/2011

g Discovery – Overview 13

3.1 Introduction 13

3.2 GPCR in the Human Genome 14

3.2.1 Introduction 14

3.2.2 The Traditional Classification System 14

3.2.3 The GRAFS Classification System 15

3.3 Structure of GPCRs 17

3.3.1 General Structure 17

3.3.2 Importance of the 7TM 17

3.4 Structure of G-proteins 18

3.5 Coupling to G-proteins 19

3.5.1 Introduction 19

3.5.2 The Signal Transduction Pathways Involving GPCR 19

3.6 Second Messengers in the GPCR System 22

3.6.1 Introduction to Second Messengers 22

3.6.2 Cyclic Adenosine Monophosphate (cAMP) 22

3.6.3 Cyclic Guanosine Monophosphate (cGMP) 23

3.6.4 Diacylglycerol (DAG) 23

3.6.5 Inositol 1, 4, 5-triphosphate (IP3) 24

3.6.6 Calcium Ions (Ca2+ ) 24

3.7 Post-Translational Modifications 25

3.7.1 Glycosylation, Palmitoylation and Phosphorylation 25

3.7.2 GPCR Desensitization 25

4 GPCRs in Drug Discovery – Novel Research Methods in GPCR Drug Discovery 26

4.1 Introduction 26

4.2 Structure-Based Research in GPCR 26

4.2.1 Introduction 26

4.2.2 New Avenues 26

4.2.3 Case Studies 27

4.3 Fragment-Based Drug Discovery 28

4.3.1 Introduction 28

4.3.2 New Avenues 28

4.3.3 Case Study 28

4.4 Ligand-Induced Selective Signaling (LiSS) 28

4.4.1 Introduction 28

4.4.2 New Avenues 29

4.4.3 Case Study 29

4.5 Allosterism and GPCRs 29

4.5.1 Introduction 29

4.5.2 New Avenues 30

4.5.3 Case Studies 31

4.6 GPCR Dimerization 32

4.6.1 Introduction 32

4.6.2 Need to Form Dimers 32

4.6.3 New Avenues 32

4.6.4 Case Studies 33

4.7 GPCR Oligomerization 34

4.7.1 Introduction 34

4.7.2 Classification of Oligomers 34

4.7.3 New Avenues 35

4.7.4 Case Studies 35

5 GPCRs in Drug Discovery – Orphan GPCRs
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