Abstract
Sphingolipids are membrane lipids that play important roles in the regulation of cell functions and homeostasis. Alterations in their metabolism have been associated with several pathologies. For this reason, therapeutic strategies based on the design of small molecules to restore sphingolipid levels to their physiological condition have rapidly emerged. In addition, some of these new chemical entities, even if they fail to succeed along the pipeline, can become valuable pharmacological tools for the study of sphingolipid function. Implications of altered sphingolipid metabolism in cancer progression have allowed the identification of new targets for the development of potential anticancer agents. Based on these premises, this review is focused on the most recent achievements in the field, with special attention to the development of small molecules, mainly enzyme inhibitors, able to disrupt some of the key sphingolipid metabolic pathways implicated in cancer progression. On the other hand, metabolic dysregulation can also be modulated by the use of sphingolipid analogs, which can alter the sphingolipid balance driving cells to death or survival and thus becoming useful candidates for subsequent drug development.
Keywords: Sphingolipids, Enzyme inhibitors, Analogs, Modulation, Metabolism, dhCer, cyclopropane, Cer-recognizing factors, denocarcinoma
Anti-Cancer Agents in Medicinal Chemistry
Title:Sphingolipid Modulation: A Strategy for Cancer Therapy
Volume: 12 Issue: 4
Author(s): Antonio Delgado, Gemma Fabrias, Carmen Bedia, Josefina Casas and Jose Luis Abad
Affiliation:
Keywords: Sphingolipids, Enzyme inhibitors, Analogs, Modulation, Metabolism, dhCer, cyclopropane, Cer-recognizing factors, denocarcinoma
Abstract: Sphingolipids are membrane lipids that play important roles in the regulation of cell functions and homeostasis. Alterations in their metabolism have been associated with several pathologies. For this reason, therapeutic strategies based on the design of small molecules to restore sphingolipid levels to their physiological condition have rapidly emerged. In addition, some of these new chemical entities, even if they fail to succeed along the pipeline, can become valuable pharmacological tools for the study of sphingolipid function. Implications of altered sphingolipid metabolism in cancer progression have allowed the identification of new targets for the development of potential anticancer agents. Based on these premises, this review is focused on the most recent achievements in the field, with special attention to the development of small molecules, mainly enzyme inhibitors, able to disrupt some of the key sphingolipid metabolic pathways implicated in cancer progression. On the other hand, metabolic dysregulation can also be modulated by the use of sphingolipid analogs, which can alter the sphingolipid balance driving cells to death or survival and thus becoming useful candidates for subsequent drug development.
Export Options
About this article
Cite this article as:
Delgado Antonio, Fabrias Gemma, Bedia Carmen, Casas Josefina and Abad Jose Luis, Sphingolipid Modulation: A Strategy for Cancer Therapy, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (4) . https://dx.doi.org/10.2174/187152012800228643
DOI https://dx.doi.org/10.2174/187152012800228643 |
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
-
Molecular Imaging of Therapeutic Potential of Reporter Probes
Current Drug Targets Lipophilicity and Other Parameters Affecting Brain Penetration
Current Medicinal Chemistry - Central Nervous System Agents Contextualizing the Genes Altered in Bladder Neoplasms in Pediatric and Teen Patients Allows Identifying Two Main Classes of Biological Processes Involved and New Potential Therapeutic Targets
Current Genomics Neuro-Transmitters in the Central Nervous System & their Implication in Learning and Memory Processes
Current Medicinal Chemistry The Emerging Role of EMT-related lncRNAs in Therapy Resistance and their Applications as Biomarkers
Current Medicinal Chemistry Inhibition of Human 5-Lipoxygenase and Anti-Neoplastic Effects by 2-Amino-1,4-Benzoquinones
Medicinal Chemistry Imaging of EGFR and EGFR Tyrosine Kinase Overexpression in Tumors by Nuclear Medicine Modalities
Current Pharmaceutical Design Radiolabeled Nanoparticles for Cancer Diagnosis and Therapy
Anti-Cancer Agents in Medicinal Chemistry Editorial Review 2017
Current Radiopharmaceuticals Drug Targeting of Estrogen Receptor Signaling in the Cardiovascular System: Preclinical and Clinical Studies
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Concepts for Nano-delivery of Therapeutic Immunomodulatory Agents
Current Bionanotechnology (Discontinued) The First Total Synthesis of Tarennane, a Potent Antioxidant Chalcone Constituent from Tarenna Attenuate or Magnolia Officinalis
Letters in Organic Chemistry Recent Advances in Radiation Therapy of Cancer Cells: A Step towards an Experimental and Systems Biology Framework
Current Radiopharmaceuticals RNA Interference-Mediated Validation of Survivin and Apollon/BRUCE as New Therapeutic Targets for Cancer Therapy
Current Topics in Medicinal Chemistry Targeting Molecular Imaging of Breast Cancer by Radioimmunodetection Method in Nuclear Medicine
Current Molecular Imaging (Discontinued) Perspectives on Medicinal Properties of Mangiferin
Mini-Reviews in Medicinal Chemistry Gold and Silver Nanoparticles for Applications in Theranostics
Current Topics in Medicinal Chemistry Epidemiology, Clinical Presentation and Treatment of Mucosal Melanoma
Clinical Cancer Drugs Targeting Angiogenesis in Renal Cell Carcinoma
Current Cancer Drug Targets Meet Our Editorial Board Member
Current Protein & Peptide Science