Abstract
Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.
Keywords: Anti-cancer agents, protein kinase inhibitors, drug design, active kinase conformation, nactive kinase conformation, selectivity, inactive kinase conformation
Mini-Reviews in Medicinal Chemistry
Title: Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance
Volume: 6 Issue: 10
Author(s): R. Griffith, M. N. Brown, A. McCluskey and L. K. Ashman
Affiliation:
Keywords: Anti-cancer agents, protein kinase inhibitors, drug design, active kinase conformation, nactive kinase conformation, selectivity, inactive kinase conformation
Abstract: Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.
Export Options
About this article
Cite this article as:
Griffith R., N. Brown M., McCluskey A. and K. Ashman L., Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance, Mini-Reviews in Medicinal Chemistry 2006; 6 (10) . https://dx.doi.org/10.2174/138955706778560184
DOI https://dx.doi.org/10.2174/138955706778560184 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
- 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
Related Articles
-
Safer Vectors for Gene Therapy of Primary Immunodeficiencies
Current Gene Therapy DNA Mismatch Repair Deficiency, Resistance to Cancer Chemotherapy and the Development of Hypersensitive Agents
Current Topics in Medicinal Chemistry Growth and Trophic Factors, pH and the Na+/H+ Exchanger in Alzheimers Disease, Other Neurodegenerative Diseases and Cancer: New Therapeutic Possibilities and Potential Dangers
Current Alzheimer Research Tyrphostins as Potential Therapeutic Agents for Acute Kidney Injury
Current Medicinal Chemistry Signaling Intermediates (PI3K/PTEN/AKT/mTOR and RAF/MEK/ERK Pathways) as Therapeutic Targets for Anti-Cancer and Anti-Angiogenesis Treatments
Current Signal Transduction Therapy Immunogenic Issues Concerning Recombinant Adeno-Associated Virus Vectors for Gene Therapy
Current Gene Therapy Breast Cancer: Understanding Sensitivity and Resistance to Chemotherapy and Targeted Therapies to Aid in Personalised Medicine
Current Cancer Drug Targets Synthesis and Biological Evaluation of 2-, 3-, and 4-Acylaminocinnamyl-Nhydroxyamides as Novel Synthetic HDAC Inhibitors
Medicinal Chemistry Challenges in the Management of Paediatric Febrile Neutropenia
Current Pediatric Reviews Caffeic Acid Phenethyl Ester Effects: In Silico Study of its Osteoimmunological Mechanisms
Letters in Drug Design & Discovery Can Breast Cancer Stem Cells Evade the Immune System?
Current Medicinal Chemistry Is Going for Cure in CML Targeting Aberrant Glycogen Synthase Kinase 3β?
Current Drug Targets MICA Molecules in Disease and Transplantation, a Double-Edged Sword?
Current Immunology Reviews (Discontinued) The Tachykinergic System as Avenues for Drug Intervention
Recent Patents on CNS Drug Discovery (Discontinued) A Review on Exploring Better Safety Prospects in Managing Cancer using Liposomal Combinations of Food Bioactive Compounds and Anticancer Drugs: Combisomes
Current Drug Delivery Applications of Nanosystems to Anticancer Drug Therapy (Part II. Dendrimers, Micelles, Lipid-based Nanosystems)
Recent Patents on Anti-Cancer Drug Discovery Stem Cell Genetic Therapy for Fanconi Anemia – A New Hope
Current Gene Therapy Cyclin-Dependent Kinase Inhibitors as Anticancer Drugs
Current Drug Targets Hck Inhibitors as Potential Therapeutic Agents in Cancer and HIV Infection
Current Medicinal Chemistry Two Promising Anti-Cancer Compounds, 2-Hydroxycinnaldehyde and 2- Benzoyloxycinnamaldehyde: Where do we stand?
Combinatorial Chemistry & High Throughput Screening