Glycogen Synthase Kinase 3 (GSK-3) and Its

Many researchers believe that GSK-3 and its inhibitors could lead to effective treatments for neurogenerative disorders, type II diabetes, depression and bipolar disorder, and some forms of cancer. This book provides a thorough introduction to GSK-3, presents up-to-date information, and mentions the birth of several chemical families of GSK-3 inhibitors with varying selectivity. It's a great reference for researchers in drug design and development.

ANA MARTINEZ is the Research and Development Director for NeuroPharma. She has been and still is an active researcher in the design and synthesis of GSK-3 inhibitors.

ANA CASTRO is the Medicinal Chemistry Director of NeuroPharma. She was formerly a tenured scientist at the Medicinal Chemistry Institute.

MIGUEL MEDINA is the Drug Discovery Director at NeuroPharma. He was formerly an instructor at the Brigham and Women's Hospital and the Harvard Medical School.

FOREWORD—THE ORIGINS OF GSK-3

ix

PREFACE

xvii

ACKNOWLEDGMENTS

xix

CONTRIBUTORS

xxi

ABBREVIATIONS

xxv

PART I CELLULAR FUNCTIONS OF GSK-3

1

(104)

1 Glycogen Synthase Kinase 3: An Introductory Synopsis

3

(22)

2 Glycogen Synthase Kinase 3&beta' (GSK-3β) a Key Signaling Enzyme: A Developmental Neurobiological Perspective

25

(20)

3 Role of GSK-3/Shaggy in Neuronal Cell Biology

45

(16)

4 The Crystal Structures of Glycogen Synthase Kinase 3

61

(22)

5 Kinase-Kinase and Site-Site Interactions in the Phosphorylation of Tau by GSK-3

83

(22)

PART II GSK-3 AS A THERAPEUTIC TARGET IN HUMAN PATHOLOGY

105

(116)

6 GSK-3, a Key Player in Alzheimer's Disease

107

(18)

7 Glycogen Synthase Kinase 3: A Target for Novel Mood Disorder Treatments

125

(30)

8 GSK-3 and Stem Cells

155

(18)

9 Glycogen Synthase Kinase 3: Role in Neurodegeneration and Neuroprotection

173

(16)

10 Protein Kinase Assays for Drug Discovery

189

(14)

11 Animal Models with Modified Expression of GSK-3 for the Study of Its Physiology and of Its Implications in Human Pathologies

203

(18)

PART III GSK-3 INHIBITORS: DEVELOPMENT AND THERAPEUTIC POTENTIAL

221

(112)

12 Lithium, the Seminal GSK-3 Inhibitor

223

(20)

13 Inhibition of GSK-3 as Therapeutic Strategy in Disease: Efficacy of AR-A014418

243

(14)

14 TDZD's: Selective and ATP Noncompetitive Glycogen Synthase Kinase 3 Inhibitors

257

(24)

15 3-Amino Pyrazoles as Potent and Selective Glycogen Kinase Synthase 3 (GSK-3) Inhibitors

281

(26)

16 Marine Compounds as a New Source for Glycogen Synthase Kinase 3 Inhibitors

307

(26)

INDEX

333

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Glycogen Synthase Kinase 3 (GSK-3) and Its Inhibitors Drug Discovery and Development

Summary

Author Biography

Table of Contents

Supplemental Materials