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
-
Retinoic Acid and Iron Metabolism: A Step Towards Design of a Novel Antitubercular Drug
Current Pharmaceutical Biotechnology Survivin: Role in Normal Cells and in Pathological Conditions
Current Cancer Drug Targets Histone Deacetylase Inhibitors in the Treatment of Hematological Malignancies
Mini-Reviews in Medicinal Chemistry Safer Vectors for Gene Therapy of Primary Immunodeficiencies
Current Gene Therapy Chemical Metabolic Inhibitors for the Treatment of Blood-Borne Cancers
Anti-Cancer Agents in Medicinal Chemistry Chemotherapeutic Effects of Acridine Derivatives
Medicinal Chemistry Reviews - Online (Discontinued) Copper Compounds in Cancer Chemotherapy
Current Medicinal Chemistry Advances in Immunotherapy of Chronic Myeloid Leukemia CML
Current Cancer Drug Targets HIF-1α Modulates Energy Metabolism in Cancer Cells by Inducing Over-Expression of Specific Glycolytic Isoforms
Mini-Reviews in Medicinal Chemistry Nuclear Hormone Receptors and Female Reproduction
Current Molecular Medicine Immune Function in Pregnant Women with Affective Disorders
Current Psychiatry Reviews Biosafety of Onco-Retroviral Vectors
Current Gene Therapy Atomic Force Microscopy: The Characterisation of Amyloid Protein Structure in Pathology
Current Topics in Medicinal Chemistry Alteration of the Proline at Position 7 of the HIV-1 Spacer Peptide p1 Suppresses Viral Infectivity in a Strain Dependent Manner
Current HIV Research Signal Transduction and Photodynamic Therapy
Current Signal Transduction Therapy Doxsaliform: A Novel N-Mannich Base Prodrug of a Doxorubicin Formaldehyde Conjugate
Letters in Drug Design & Discovery Posttranslational Regulation of O6-Methylguanine-DNA Methyltransferase (MGMT) and New Opportunities for Treatment of Brain Cancers
Mini-Reviews in Medicinal Chemistry Targeting Kinase-activating Genetic Lesions to Improve Therapy of Pediatric Acute Lymphoblastic Leukemia
Current Medicinal Chemistry Tipping the Balance Between Life and Death: Targeting Histone Acetylation for Cancer Therapy
Drug Delivery Letters Molecular Imaging of Apoptosis with Radio-Labeled Annexin A5 Focused on the Evaluation of Tumor Response to Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry