TY - BOOK ID - 5451196 TI - Protein tyrosine kinases : from inhibitors to useful drugs AU - Fabbro, D. AU - McCormick, Frank PY - 2006 SN - 9781588293848 158829384X 9781592599622 9786610358779 1280358777 1592599621 PB - Totowa, N.J. : Humana Press, DB - UniCat KW - Protein-Tyrosine Kinase KW - Lymphocyte Specific Protein Tyrosine Kinase p56(lck) KW - Neoplasms KW - src-Family Kinases KW - Protein-tyrosine kinase KW - Cancer KW - physiology. KW - drug therapy. KW - Inhibitors KW - Therapeutic use. KW - Chemotherapy. KW - Chimiothérapie KW - Cancer -- Chemotherapy. KW - Protein-tyrosine kinase -- Inhibitors -- Therapeutic use. KW - Biology KW - Medicine KW - Chemistry KW - Physical Sciences & Mathematics KW - Health & Biological Sciences KW - Biochemistry KW - Cytology KW - Oncology KW - Biology - General KW - Therapeutic use KW - Chemotherapy KW - Hydroxyaryl-protein kinase KW - Tyrosine kinase KW - Tyrosine protein kinase KW - Tyrosine-specific protein kinase KW - Tyrosylprotein kinase KW - Life sciences. KW - Biochemistry. KW - Life Sciences. KW - Biochemistry, general. KW - Protein kinases KW - Antineoplastic agents KW - Treatment UR - https://www.unicat.be/uniCat?func=search&query=sysid:5451196 AB - Protein kinases function as components of signal transduction pathways, playing a central role in the control of cell growth, metabolism, differentiation, and apoptosis. The development of selective protein tyrosine kinase (PTK) inhibitors that can block or modulate diseases, such as cancer, with abnormalities in these signaling pathways is considered a promising approach for drug development. Currently, more than 20 different PTKs are being considered as potential therapeutic targets in oncology. In Protein Tyrosine Kinases: From Inhibitors to Useful Drugs, leading researchers from the Novartis group that pioneered Gleevec/Glivec™ and from around the world comprehensively survey the state-of-the-art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made toward generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing PTK inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors. Authoritative and state-of-the-art, Protein Tyrosine Kinases: From Inhibitors to Useful Drugs details the key stages in the design of PTK inhibitors and their development into useful drugs. ER -