Abstract
With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry for treating tumours caused by kinase malfunctioning. Among different types of kinase inhibitors, the design of Type II inhibitors has been rationalized for maximizing the benefits and reducing drawbacks. Here we highlight the development made in Type II inhibitors, discussing the advantages and disadvantages of these types of molecules. Furthermore, we present the strategies for designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.
Keywords: Allosteric inhibitors, cancer, covalent inhibitors, DFG-in, DFG-out, kinase inhibitors, Type I inhibitors, Type II inhibitors, Type III inhibitors, Type IV inhibitors.
Anti-Cancer Agents in Medicinal Chemistry
Title:Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design
Volume: 13 Issue: 5
Author(s): Javier Blanc, Raphael Geney and Christel Menet
Affiliation:
Keywords: Allosteric inhibitors, cancer, covalent inhibitors, DFG-in, DFG-out, kinase inhibitors, Type I inhibitors, Type II inhibitors, Type III inhibitors, Type IV inhibitors.
Abstract: With the advent of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has brought a revolution in medicinal chemistry for treating tumours caused by kinase malfunctioning. Among different types of kinase inhibitors, the design of Type II inhibitors has been rationalized for maximizing the benefits and reducing drawbacks. Here we highlight the development made in Type II inhibitors, discussing the advantages and disadvantages of these types of molecules. Furthermore, we present the strategies for designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.
Export Options
About this article
Cite this article as:
Blanc Javier, Geney Raphael and Menet Christel, Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design, Anti-Cancer Agents in Medicinal Chemistry 2013; 13 (5) . https://dx.doi.org/10.2174/1871520611313050008
DOI https://dx.doi.org/10.2174/1871520611313050008 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Nutritional Status and Lipid Profile in HIV-Infected Adults
Endocrine, Metabolic & Immune Disorders - Drug Targets Regulatory T Cells in Cancer Biology: A Possible New Target for Biochemical Therapies
Mini-Reviews in Medicinal Chemistry Epigenetic Effects of Environmental Chemicals on Reproductive Biology
Current Drug Targets Molecular Imaging in Optical Coherence Tomography
Current Molecular Imaging (Discontinued) Synthesis of Tetrahydrobenzo[b]thiophene-3-carbohydrazide Derivatives as Potential Anti-cancer Agents and Pim-1 Kinase Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Biologic Therapy in Inflammatory and Immunomediated Arthritis: Safety Profile
Current Drug Safety Mitochondrial Uncoupling and the Regulation of Glucose Homeostasis
Current Diabetes Reviews Mechanisms Involved in the Development of Chronic Hepatitis C as Potential Targets of Antiviral Therapy
Current Pharmaceutical Biotechnology In Silico Machine Learning Methods in Drug Development
Current Topics in Medicinal Chemistry Synthesis and Antitumor Activity of Novel 4-Chloro-3-Arylmaleimide Derivatives
Letters in Drug Design & Discovery Future Treatment for COPD: Targeting Oxidative Stress and its Related Signal
Recent Patents on Inflammation & Allergy Drug Discovery An Investigative Approach to Treatment Modalities for Squamous Cell Carcinoma of Skin
Current Drug Delivery Curcumin: the Yellow Molecule with Pleiotropic Biological Effects
Letters in Drug Design & Discovery Editorial (Thematic Issue: Bioinformatics and Biotechnology)
Current Biotechnology Emerging Strategies in Stimuli-Responsive Nanocarriers as the Drug Delivery System for Enhanced Cancer Therapy
Current Pharmaceutical Design Patent Review on Nanotechnology in Ocular Drug Delivery
Recent Patents on Nanomedicine Pharmacogenetics of the Cytochromes P450
Current Topics in Medicinal Chemistry Experimental Onco-Immunology Revisited
Current Cancer Therapy Reviews Complexity in Clinical Trials: Blind Spots, Misleading Criteria, Winners and Losers
Clinical Cancer Drugs PI3K-Akt Signaling and Viral Infection
Recent Patents on Biotechnology