000 03798nam a22004575i 4500
001 978-1-59259-962-2
003 DE-He213
005 20161121230702.0
007 cr nn 008mamaa
008 100301s2006 xxu| s |||| 0|eng d
020 _a9781592599622
_9978-1-59259-962-2
024 7 _a10.1385/1592599621
_2doi
050 4 _aQH345
050 4 _aQD415-436
072 7 _aPSB
_2bicssc
072 7 _aSCI007000
_2bisacsh
082 0 4 _a572
_223
245 1 0 _aProtein Tyrosine Kinases
_h[electronic resource] :
_bFrom Inhibitors to Useful Drugs /
_cedited by Doriano Fabbro, Frank McCormick.
264 1 _aTotowa, NJ :
_bHumana Press,
_c2006.
300 _aXIII, 290 p.
_bonline resource.
336 _atext
_btxt
_2rdacontent
337 _acomputer
_bc
_2rdamedia
338 _aonline resource
_bcr
_2rdacarrier
347 _atext file
_bPDF
_2rda
490 1 _aCancer Drug Discovery and Development
505 0 _aProtein Tyrosine Kinases as Targets for Cancer and Other Indications -- Inhibitors of Signaling Interfaces -- PI3-Kinase Inhibition -- Src as a Target for Pharmaceutical Intervention -- Activated FLT3 Receptor Tyrosine Kinase as a Therapeutic Target In Leukemia -- JAK Kinases in Leukemias, Lymphomas, and Multiple Myeloma -- Glivec® (Gleevec®, Imatinib, STI571) -- Platelet-Derived Growth Factor -- Structural Biology of Protein Tyrosine Kinases -- Testing of Signal Transduction Inhibitors in Animal Models of Cancer -- Phosphoproteomics in Drug Discovery and Development.
520 _aProtein 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.
650 0 _aLife sciences.
650 0 _aBiochemistry.
650 1 4 _aLife Sciences.
650 2 4 _aBiochemistry, general.
700 1 _aFabbro, Doriano.
_eeditor.
700 1 _aMcCormick, Frank.
_eeditor.
710 2 _aSpringerLink (Online service)
773 0 _tSpringer eBooks
776 0 8 _iPrinted edition:
_z9781588293848
830 0 _aCancer Drug Discovery and Development
856 4 0 _uhttp://dx.doi.org/10.1385/1592599621
912 _aZDB-2-SBL
950 _aBiomedical and Life Sciences (Springer-11642)
999 _c502441
_d502441