Abstract
This article reviews several important observations in the field of protein kinase drug discovery, exemplified mainly by targeting c-Abl for the treatment of CML. Structure-based strategy and insight are provided for the optimization of the selectivity and resistant mutation profiles of protein kinase inhibitors.
Keywords: Protein kinase, protein kinase inhibitor, selectivity, imatinib, CML, drug-resistant mutation, systematic structural analysis
Current Topics in Medicinal Chemistry
Title: Molecular Targeting of Protein Kinases to Optimize Selectivity and Resistance Profiles of Kinase Inhibitors
Volume: 7 Issue: 14
Author(s): Liao Jie-Lou Jeffrey
Affiliation:
Keywords: Protein kinase, protein kinase inhibitor, selectivity, imatinib, CML, drug-resistant mutation, systematic structural analysis
Abstract: This article reviews several important observations in the field of protein kinase drug discovery, exemplified mainly by targeting c-Abl for the treatment of CML. Structure-based strategy and insight are provided for the optimization of the selectivity and resistant mutation profiles of protein kinase inhibitors.
Export Options
About this article
Cite this article as:
Jeffrey Jie-Lou Liao, Molecular Targeting of Protein Kinases to Optimize Selectivity and Resistance Profiles of Kinase Inhibitors, Current Topics in Medicinal Chemistry 2007; 7 (14) . https://dx.doi.org/10.2174/156802607781696800
DOI https://dx.doi.org/10.2174/156802607781696800 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
The Yin and Yang of CD4+ Regulatory T Cells in Autoimmunity and Cancer
Current Medicinal Chemistry The Mutator Phenotype in Cancer: Molecular Mechanisms and Targeting Strategies
Current Drug Targets Resveratrol, a Phytochemical Inducer of Multiple Cell Death Pathways: Apoptosis, Autophagy and Mitotic Catastrophe
Current Medicinal Chemistry Targeting Cancer Cells by an Oxidant-Based Therapy
Current Molecular Pharmacology In vitro Measurement and In vivo Prediction of Time-Dependent Inhibitory Effects of Three Tyrosine Kinase Inhibitors on CYP3A Activity
Current Drug Metabolism Current Development of ROS-Modulating Agents as Novel Antitumor Therapy
Current Cancer Drug Targets New Strategies in the Discovery of Novel Non-Camptothecin Topoisomerase I Inhibitors
Current Medicinal Chemistry Emerging RNA-based Drugs: siRNAs, microRNAs and Derivates
Central Nervous System Agents in Medicinal Chemistry Novel Therapeutic Agents Against Cancer Stem Cells of Chronic Myeloid Leukemia
Anti-Cancer Agents in Medicinal Chemistry Immunotherapy for Alzheimers Disease: Rational Basis in Ongoing Clinical Trials
Current Pharmaceutical Design Forodesine (BCX-1777, Immucillin H) - A New Purine Nucleoside Analogue: Mechanism of Action and Potential Clinical Application
Mini-Reviews in Medicinal Chemistry Signaling Mechanism for the Insulin-like Effects of Growth Hormone - Another Example of a Classical Hormonal Negative Feedback Loop
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Recent Developments of DNA Poisons - Human DNA Topoisomerase IIα Inhibitors - as Anticancer Agents
Current Pharmaceutical Design Intriguing Classes of Acridine Derivatives as DNA-binding Antitumour Agents: From Pyrimido[5,6,1-de]acridines to Bis(acridine-4-carboxamides)
Medicinal Chemistry Reviews - Online (Discontinued) Novel Aspects of Natural and Modified Vinca Alkaloids
Current Medicinal Chemistry - Anti-Cancer Agents Synthesis and Anticancer Activity of Some 2-[3/4-(2-Substituted Phenyl-2- oxoethoxy)benzylidene]-6-substituted-2,3-dihydro-1H-inden-1-one Derivatives
Letters in Drug Design & Discovery Bcl-2 Inhibitors: Emerging Drugs in Cancer Therapy
Current Medicinal Chemistry Glyoxalase 1 and 2 Enzyme Inhibitory Activity of 6-Sulfamoylsaccharin and Sulfocoumarin Derivates
Letters in Drug Design & Discovery The Chemistry and Bio-Medicinal Significance of Pyrimidines & Condensed Pyrimidines
Current Topics in Medicinal Chemistry Natural Small Molecules as Stabilizers and Activators of Cancer-Associated NQO1 Polymorphisms
Current Drug Targets