Ana Martinez & Ana Castro 
Glycogen Synthase Kinase 3 (GSK-3) and Its Inhibitors 
Drug Discovery and Development

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.

Table des matières

Foreword: The Origins of GSK-3.

Preface.

Acknowledgments.

Contributors.

Abbreviations.

PART I: CELLULAR FUNCTIONS OF GSK-3.

1. Glycogen Synthase Kinase-3 – an Introductory Synopsis .

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

3. Role of GSK3/Shaggy in neuronal cell biology.

4. The Crystal Structures of Glycogen Synthase Kinase 3.

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

PART II: GSK3 AS A THERAPEUTIC TARGET IN HUMAN PATHOLOGY.

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

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

8. GSK3 and Stem Cells.

9. Glycogen Synthase Kinase-3: role in Neurodegeneration and Neuroprotection.

10. Protein Kinase Inhibitors. Assay Development.

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

PART III: GSK-3 INHIBITORS: DEVELOPMENT AND THERAPEUTIC POTENTIAL.

12. Lithium, the Seminal GSK3 Inhibitor.

13. Inhibition of GSK3 as Therapeutic Strategy in Disease: Efficacy of AR-A014418.

14. TDZD’s: Selective And ATP Non Competitive Glycogen Synthase Kinase-3 Inhibitors.

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

16. Marine compounds as a new source for Glycogen Synthase Kinase-3 Inhibitors.

Index.

A propos de l’auteur

ANA MARTINEZ is the Research and Development Director for
Neuro Pharma. 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
Neuro Pharma. She was formerly a tenured scientist at the Medicinal
Chemistry Institute.

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