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 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
The PA207 Peptide Inhibitor of LIM-only Protein 2 (Lmo2) Targets Zinc Finger Domains in a Non-specific Manner
Protein & Peptide Letters Anti-Tumour Activity of Glycodendrimer Nanoparticles in a Subcutaneous MEC-1 Xenograft Model of Human Chronic Lymphocytic Leukemia
Anti-Cancer Agents in Medicinal Chemistry Challenging the Current Approaches to Multiple Myeloma-Related Bone Disease: From Bisphosphonates to Target Therapy
Current Cancer Drug Targets MicroRNAs in Chronic Lymphocytic Leukemia: An Old Disease with New Genetic Insights
MicroRNA New Perspective on the Dual Functions of Indirubins in Cancer Therapy and Neuroprotection
Anti-Cancer Agents in Medicinal Chemistry Synthesis and Evaluation of A New Series of Thiazole Derivatives as Potential Antitumor Agents and MMP Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Nontoxic-dose of Deguelin Induce NPMc+ AML Cell Differentiation by Selectively Targeting Mt NPM1/SIRT1 Instead of HDAC1/3
Current Cancer Drug Targets 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 Targeting Prostate Cancer Stem Cells
Anti-Cancer Agents in Medicinal Chemistry Immunotherapy for Myeloproliferative Neoplasms (MPN)
Current Cancer Drug Targets Leptin, Ciliary Neurotrophic Factor, Leukemia Inhibitory Factor and Interleukin- 6: Class-I Cytokines Involved in the Neuroendocrine Regulation of the Reproductive Function
Current Protein & Peptide Science Pharmacophore Modelling as a Virtual Screening Tool for the Discovery of Small Molecule Protein-protein Interaction Inhibitors
Current Pharmaceutical Design Receptor Tyrosine Kinases Take a Direct Route to Mitochondria: An Overview
Current Protein & Peptide Science Targeting Ion Channels in Leukemias: A New Challenge for Treatment
Current Medicinal Chemistry Emerging Roles for Modulation of microRNA Signatures in Cancer Chemoprevention
Current Cancer Drug Targets Unleashing the Guardian: The Targetable BCR-ABL/HAUSP/PML/PTEN Network in Chronic Myeloid Leukemia
Current Drug Targets PDE-5 Inhibitors for BPH-Associated LUTS
Current Drug Targets Reconceptualizing Adult Neurogenesis: Role for Sphingosine-1-Phosphate and Fibroblast Growth Factor-1 in Co-Ordinating Astrocyte-Neuronal Precursor Interactions
CNS & Neurological Disorders - Drug Targets Regulation and Function of DNA and Histone Methylations
Current Pharmaceutical Design Novel Therapeutic Agents Against Cancer Stem Cells of Chronic Myeloid Leukemia
Anti-Cancer Agents in Medicinal Chemistry