Targeting Protein Kinases for Cancer Therapy

David J. Matthews 지음

Wiley 2011년 09월 20일 출간

작품소개

책소개

An expert guide to targeting protein kinases in cancer therapyResearch has shown that protein kinases can instigate the formation and spread of cancer when they transmit faulty signals inside cells. Because of this fact, pharmaceutical scientists have targeted kinases for intensive study, and have been working to develop medicinal roadblocks to sever their malignant means of communication.Complete with full-color presentations, Targeting Protein Kinases for Cancer Therapy defines the structural features of protein kinases and examines their cellular functions. Combining kinase biology with chemistry and pharmacology applications, this book enlists emerging data to drive the discovery of new cancer-fighting drugs. Valuable information includes:Comprehensive overviews of the major kinase families involved in oncology, integrating protein structure and function, and providing important tools to assist pharmaceutical researchers to understand and work in this dynamic area of cancer drug researchFocus on small molecule inhibitors as well as other therapeutic modalitiesDiscussion of kinase inhibitors that have entered clinical trials for the treatment of cancer, with an emphasis on molecules that have progressed to late stage clinical trials and, in a few cases, to marketProviding a platform for further study, this important work reviews both the successes and challenges of kinase inhibitor therapy, and provides insight into future directions in the war against cancer.

목차

Preface.Acknowledgments.1 KINASES AND CANCER.1.1 A Brief History of Protein Phosphorylation.1.2 Kinases and Cancer.1.3 A Tour of the Human Protein Kinase Superfamily.1.3.1 Tyrosine Kinase Group.1.3.2 TKL (Tyrosine Kinase-Like) Group.1.3.3 STE Group.1.3.4 CSNK1 Group.1.3.5 AGC group.1.3.6 CAMK Group.1.3.7 CMGC Group.1.3.8 RGC Group.1.3.9 Others.1.3.10 Atypical Protein Kinases.1.3.11 Non-Protein Kinases.1.4 Strategic Considerations for Selecting Kinases as Drug Targets.1.5 Comparison of Kinase Inhibitor Therapeutic Strategies.1.5.1 Small Molecule Versus Antibody-Directed Therapies.1.5.2 Alternative Strategies for Kinase Inhibition.References.2 PROTEIN KINASE STRUCTURE, FUNCTION AND REGULATION.2.1 Ligand Binding to Receptor Tyrosine Kinases.2.1.1 EGF:EGF Receptor Interactions.2.1.2 Insulin:Insulin Receptor and IGF1:IGF1R.2.1.3 FGF:FGF Receptor (Heparin/Heparan Sulphate) Interactions.2.1.4 VEGF:VEGF Receptor Interactions.2.1.5 Angiopoietin2:TIE2 Receptor Interactions.2.1.6 Ephrin:EPH Receptor Interactions.2.1.7 The Role of Transmembrane Domains.2.2 Protein Kinase Domain Structure and Function.2.3 Catalytic Activity of Protein Kinases.2.3.1 Steady State Kinetics.2.3.2 Chemistry of Protein Kinase Catalysis.2.4 Protein Kinase Regulation.2.4.1 Regulation Via Activation Segment Phosphorylation.2.4.2 Regulation by N-terminal Sequences and Domains.2.4.3 C-Terminal Regulatory Regions.2.4.4 Regulation by Other Domains and Partner Proteins.References.3 RECPETOR TYROSINE KINASES.3.1 EGF/ERBB Receptors.3.1.1 ERBB Receptors and Cancer.3.2 Insulin/IGF Receptors.3.2.1 Insulin/IGF Receptors and Cancer.3.3 Anaplastic Lymphoma Kinase.3.3.1 ALK and Cancer.3.4 VEGF Receptors (VEGFR1, VEGFR2, VEGFR3).3.5 PDGF Receptors.3.5.1 PDGFRs and Cancer.3.6 FGF Receptors.3.6.1 FGFRs and Cancer.3.7 KIT.3.7.1 KIT and Cancer

출판사 서평

"The comprehensive coverage makes the book highly recommendable for beginners and expert researchers in oncology and should be present on their shelves." (ChemMedChem, November 2010)

작가정보

저자(글) David J. Matthews

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DAVID J. MATTHEWS is Executive Director of Oncology Discovery at Exelixis, where he is responsible for cancer drug discovery. For more than fifteen years, Dr. Matthews has been involved in drug discovery projects in industry, with particular focus on small molecule inhibitors. He has twenty scientific publications and multiple patents to his credit.MARY E. GERRITSEN is Vice President of Molecular and Cellular Pharmacology at Exelixis, where she is in charge of cell-based screening in preclinical research and of biomarker studies for clinical development compounds in Phase I and II studies. Her prior industry experience includes positions at Genentech, Bayer and Millennium Pharmaceuticals. She has authored more than one hundred peer-reviewed articles and twenty-six book chapters and is an inventor on forty-two issued patents.