Abstract
Cancer is a serious disease characterized by the uncontrolled growth division of cells, and nowadays it remains a significant challenge for the medical field. Malaria is an infectious disease in the similar situation to cancer. Almost 40% people in the world live in areas with malaria risk and each year there are about 2 to 3 million people dying from malaria. Farnesyltransferase (FTase) that belongs to isoprenyltransferase family can catalyze the initial step of Ras-processing and is identified as a promising target for the treatment of cancer and malaria. During the past decade years, a large number of FTase inhibitors with anticancer or antimalarial activity have been reported and some of them are undergoing clinical development. This review mainly introduces the FTase inhibitors as anticancer and antimalarial agents, with focus on their enzyme inhibitory activity, stability and enzyme selectivity, etc. In particular, the promising new FTase inhibitors among them will be discussed in detail and the inspirations for their design will be highlighted.
Keywords: Anticancer, antimalaria, farnesyltransferase, FTase inhibitors, FTase inhibitory activity, selectivity.
Mini-Reviews in Medicinal Chemistry
Title:The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents
Volume: 15 Issue: 10
Author(s): Yan Shen, Shengsheng Qiang and Shutao Ma
Affiliation:
Keywords: Anticancer, antimalaria, farnesyltransferase, FTase inhibitors, FTase inhibitory activity, selectivity.
Abstract: Cancer is a serious disease characterized by the uncontrolled growth division of cells, and nowadays it remains a significant challenge for the medical field. Malaria is an infectious disease in the similar situation to cancer. Almost 40% people in the world live in areas with malaria risk and each year there are about 2 to 3 million people dying from malaria. Farnesyltransferase (FTase) that belongs to isoprenyltransferase family can catalyze the initial step of Ras-processing and is identified as a promising target for the treatment of cancer and malaria. During the past decade years, a large number of FTase inhibitors with anticancer or antimalarial activity have been reported and some of them are undergoing clinical development. This review mainly introduces the FTase inhibitors as anticancer and antimalarial agents, with focus on their enzyme inhibitory activity, stability and enzyme selectivity, etc. In particular, the promising new FTase inhibitors among them will be discussed in detail and the inspirations for their design will be highlighted.
Export Options
About this article
Cite this article as:
Shen Yan, Qiang Shengsheng and Ma Shutao, The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents, Mini-Reviews in Medicinal Chemistry 2015; 15 (10) . https://dx.doi.org/10.2174/1389557515666150511152433
DOI https://dx.doi.org/10.2174/1389557515666150511152433 |
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
-
Past, Present and Future of Nutrigenomics and its Influence on Drug Development
Current Drug Discovery Technologies Clinical Immunotherapy of B-Cell Malignancy Using CD19-Targeted CAR T-Cells
Current Gene Therapy Targeting DNA Repair Proteins: A Promising Avenue for Cancer Gene Therapy
Current Gene Therapy Targeting Translation for Treatment of Cancer - A Novel Role for IRES?
Current Cancer Drug Targets Design of New Improved Curcumin Derivatives to Multi-targets of Cancer and Inflammation
Current Drug Targets Natural Products and Cancer Stem Cells
Current Pharmaceutical Design Fusogenic Oncolytic Herpes Simplex Viruses as a Potent and Personalized Cancer Vaccine
Current Pharmaceutical Biotechnology Resveratrol: A New Potential Therapeutic Agent for Melanoma?
Current Medicinal Chemistry MicroRNAs in Cancer: Small Molecules, Big Chances
Anti-Cancer Agents in Medicinal Chemistry Disorders of Consciousness and Electrophysiological Treatment Strategies: A Review of the Literature and New Perspectives
Current Pharmaceutical Design Synthesis, Photophysical and Photochemical Aspects of Phthalocyanines for Photodynamic Therapy
Current Organic Chemistry Invariant Natural Killer T Cell-Based Therapy of Autoimmune Diseases
Current Immunology Reviews (Discontinued) Potential Therapeutic Targets of Curcumin, Most Abundant Active Compound of Turmeric Spice: Role in the Management of Various Types of Cancer
Recent Patents on Anti-Cancer Drug Discovery Synergistic Interaction of Telomerase-Specific Oncolytic Virotherapy and Chemotherapeutic Agents for Human Cancer
Current Pharmaceutical Biotechnology Thiosemicarbazone-Pt(II) Complex Causes a Growth Inhibitory Effect on Human Mesenchymal Stem Cells
Medicinal Chemistry The Importance of Drug Delivery to Optimize the Effects of Bone Morphogenetic Proteins During Periodontal Regeneration
Current Pharmaceutical Biotechnology Tumor Stroma Manipulation By MSC
Current Drug Targets Androgen Receptor Cofactors in Prostate Cancer: Potential Therapeutic Targets of Castration-Resistant Prostate Cancer
Current Cancer Drug Targets The Role of Zinc in the Treatment of Taste Disorders
Recent Patents on Food, Nutrition & Agriculture Current Trends in the Use of Cationic Polymer Assemblies for siRNA and Plasmid DNA Delivery
Pharmaceutical Nanotechnology