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 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- 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
-
Antiplatelet and Antileukocyte Effects of Cardiovascular,Immunomodulatory and Chemotherapeutic Drugs
Cardiovascular & Hematological Agents in Medicinal Chemistry Advances in Cancer Stem Cell Therapy: Targets and Treatments
Recent Patents on Regenerative Medicine Approaches to Target Profiling of Natural Products
Current Medicinal Chemistry Annotation of the Human Genome by High-Throughput Sequence Analysis of Naturally Occurring Proteins
Current Proteomics Beneficial and Adverse Effects of Molecularly Targeted Therapies for Acute Promyelocytic Leukemia in Central Nervous System
CNS & Neurological Disorders - Drug Targets Membrane Tyrosine Kinase Receptors are an Important Target for the Therapy of Acute Myeloid Leukemia
Current Cancer Therapy Reviews circEPSTI1 Acts as a ceRNA to Regulate the Progression of Osteosarcoma
Current Cancer Drug Targets Signaling in Human B-Lymphoma Rafts
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Thiopurine Biotransformation and Pharmacological Effects: Contribution of Oxidative Stress
Current Drug Metabolism Application of Mesenchymal Stem Cells in Melanoma: A Potential Therapeutic Strategy for Delivery of Targeted Agents
Current Medicinal Chemistry Anti-Apoptotic Mechanisms of Drug Resistance in Cancer
Current Cancer Drug Targets Haematopoietic Stem Cell Gene Therapy to Treat Autoimmune Disease
Current Stem Cell Research & Therapy Structural and Functional Organization of miRNAs
Current Pharmacogenomics Podophyllotoxin: Current Perspectives
Current Bioactive Compounds Polysulfated/Sulfonated Compounds for the Development of Drugs at the Crossroad of Viral Infection and Oncogenesis
Current Pharmaceutical Design Analysis of the Molecular Determinants of the Response of Chronic Myelogenous Leukaemia to Tyrosine Kinase Inhibitors
Current Pharmacogenomics Designing a Novel Multi-Epitope Vaccine Against Htlv-1 Related Adult T-cell Leukemia/Lymphoma: An In Silico Approach
Current Proteomics Some Implications of Receptor Kinase Signaling Pathway for Development of Multitargeted Kinase Inhibitors
Current Radiopharmaceuticals Nucleoside Transport as a Potential Target for Chemotherapy in Malaria
Current Pharmaceutical Design The Adipose Tissue as a Source of Vasoactive Factors
Current Medicinal Chemistry - Cardiovascular & Hematological Agents