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
Current Medicinal Chemistry - Anti-Cancer Agents
Title: Novel Oncogenic Protein Kinase Inhibitors for Cancer Therapy
Volume: 4 Issue: 5
Author(s): Tomi K. Sawyer
Affiliation:
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
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.
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Cite this article as:
Sawyer K. Tomi, Novel Oncogenic Protein Kinase Inhibitors for Cancer Therapy, Current Medicinal Chemistry - Anti-Cancer Agents 2004; 4 (5) . https://dx.doi.org/10.2174/1568011043352830
DOI https://dx.doi.org/10.2174/1568011043352830 |
Print ISSN 1568-0118 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5968 |
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