Targeting Protein Kinases for Cancer Therapy (eBook)

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.

"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)

"This excellent book is a comprehensive review of protein kinases
in the context of their roles in human cancer. ... [It] is an
excellent resource for scientists involved in selecting potential
drug targets and optimization of compounds that are likely to be
effective. The involvement of protein kinases in cancer, and
strategies for selecting drug targets is thoughtfully discussed,
and protein structures, domains and sites of regulation are
described in depth and in ways that are easy to follow and
understand. Individual kinases are described from the biological
perspective and in the context of efforts to target them, often
with case studies to illustrate specific points in exquisite
detail. Understanding these proteins at this level of detail is
essential to understand how they can be targeted and what we can
expect to observe in the clinic. Following description of the
kinases themselves and their function and regulation in signaling
pathways, and cell cycle control, the second half of this book
describes kinase inhibitors and experience gained from analyzing
these compounds in vitro and in vivo. The final chapter addresses
challenges and future directions, including issues relating to
combinational therapy and systems biology. These big issues
complete the comprehensive tour of the world of kinases in the
context of cancer, from molecular details of drug-protein
interactions, through biology to clinical application. Considering
the success so far in targeting these enzymes in the clinic, and
the level of investment currently being made to developing new
kinase inhibitors for cancer therapy, there is no doubt that this
outstanding book will be a valuable asset to the large community of
chemists, biologists and clinicians involved in developing the next
generation of therapies."

--Frank McCormick, Director, UCSF Helen Diller Family
Comprehensive Cancer Center