Current Medicinal Chemistry-Anti-Cancer Agents

Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France

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Novel Oncogenic Protein Kinase Inhibitors for Cancer Therapy

Author(s): Tomi K. Sawyer.

Abstract:

Small-molecule drug discovery for cancer therapy is making extraordinary progress within the realm of advancing novel oncogenic protein kinase inhibitor lead compounds of significant impact to both basic research and clinical testing. In this perspective, structure- and mechanism-based drug design are highlighted relative to such progress. Also, evolving concepts in novel oncogenic protein kinase inhibitor drug discovery is highlighted relative to therapeutic target selectivity, including the recent identification of oncogenic kinase mutants effecting drug-resistance or enhanced drug susceptibility to small-molecule inhibitors.

Keywords: oncogenic protein kinase, structure-based drug design, mechanism-based drug design, receptor tyrosine kinase, non-receptor tyrosine kinase, non-receptor serine/threonine kinase, atp binding site, protein kinase selectivity, sti-571, bms-354825

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Article Details

VOLUME: 4
ISSUE: 5
Year: 2004
Page: [449 - 455]
Pages: 7
DOI: 10.2174/1568011043352830
Price: $58