摘要
背景:丝氨酸-苏氨酸蛋白磷酸酶2A(PP2A)调节多种细胞信号通路并且它因病毒癌基因的失活,具体结构亚基突变或细胞的内源性抑制剂上调可能通过调节特定的磷酸化导致恶性转化。丝氨酸-苏氨酸蛋白磷酸酶2A活性药理调制成为癌症治疗的一个有吸引力的策略。一些化合物靶向丝氨酸-苏氨酸蛋白磷酸酶2A可以诱导丝氨酸-苏氨酸蛋白磷酸酶2A活化与几种类型的癌症随后的细胞死亡。 方法:我们对同行评审的文章进行了搜索书目数据库侧重于审查的主要项目。我们在发表文章索引期刊上进行选择。使用标准的文献计量指标评价检索论文的质量。 结果:纳入审查的有一百一十四篇论文。二十七篇论文给出了丝氨酸-苏氨酸蛋白磷酸酶2A的结构和生理作用的概述。二十五篇论文概述了丝氨酸-苏氨酸蛋白磷酸酶2A在肿瘤抑制的作用。四十篇论文分析了丝氨酸-苏氨酸蛋白磷酸酶2A的激活合成化合物涉及的机制,二十二篇论文概述了恢复丝氨酸-苏氨酸蛋白磷酸酶2A活性能力的天然化合物以及这可能是有益的。 结论:研究结果分析,本文强调丝氨酸-苏氨酸蛋白磷酸酶2A作为细胞生长和存活的调节中枢的作用,因此其作为肿瘤抑制。某些化合物的发现,合成或天然的,为能够激活丝氨酸-苏氨酸蛋白磷酸酶2A开辟了新的为未来策略充分利用人类癌症的治疗潜力前景。因此,本次审查也可能使制药或生物技术公司对药物设计和靶向传输特别感兴趣。
关键词: 蛋白磷酸酶2 A,癌症,芬戈莫德,硼替佐米,毛喉素,鼠尾草酸。
Current Medicinal Chemistry
Title:Pharmacological Activation of Protein Phosphatase 2 A (PP2A): A Novel Strategy to Fight Against Human Malignancies?
Volume: 23 Issue: 38
Author(s): Maria Rosaria Carratù, Anna Signorile, Domenico De Rasmo, Antonia Reale, Angelo Vacca
Affiliation:
关键词: 蛋白磷酸酶2 A,癌症,芬戈莫德,硼替佐米,毛喉素,鼠尾草酸。
摘要: Background: The serine-threonine protein phosphatase 2A (PP2A) regulates multiple cell signaling cascades and its inactivation by viral oncoproteins, mutation of specific structural subunits or upregulation of the cellular endogenous inhibitors may contribute to malignant transformation by regulating specific phosphorylation events. Pharmacological modulation of PP2A activity is becoming an attractive strategy for cancer treatment. Some compounds targeting PP2A are able to induce PP2A reactivation and subsequent cell death in several types of cancer.
Methods: We undertook a search of bibliographic databases for peer-reviewed articles focusing on the main item of the review. We selected articles published in indexed journals. The quality of retrieved papers was appraised using the standard bibliometric indicators.
Results: One hundred and fourteen papers were included in the review. Twenty-seven papers gave an overview of structure and physiological role of PP2A. Twenty-five papers outlined the role of PP2A in tumor suppression. Forty papers analyzed the mechanism involved in PP2A reactivation by synthetic compounds, and twenty-two papers outlined the capability of natural compounds of restoring PP2A activity and how this could be beneficial.
Conclusion: Findings analyzed in this review underline the central role of PP2A as a regulator of cell growth and survival, hence its function as tumor suppressor. The discovery that some compounds, either synthetic or natural, are capable of reactivating PP2A opens up new perspectives for future strategies to fully exploit therapeutic potential in human cancer. Thus, this review could also be of particular interest to pharmaceutical or biotechnology companies for drug design and targeted delivery.
Export Options
About this article
Cite this article as:
Maria Rosaria Carratù, Anna Signorile, Domenico De Rasmo, Antonia Reale, Angelo Vacca , Pharmacological Activation of Protein Phosphatase 2 A (PP2A): A Novel Strategy to Fight Against Human Malignancies?, Current Medicinal Chemistry 2016; 23 (38) . https://dx.doi.org/10.2174/0929867323666161014133423
DOI https://dx.doi.org/10.2174/0929867323666161014133423 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the Treatment of Chronic Inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
- Announcements
Related Articles
-
HDAC Inhibitors as Novel Anti-Cancer Therapeutics
Recent Patents on Anti-Cancer Drug Discovery Cyclooxygenases Regulation by Estradiol on Endothelium
Current Pharmaceutical Design Non-aspirin Non-steroidal Anti-inflammatory Drugs for the Primary Chemoprevention of Non-gastrointestinal Cancer: Summary of Evidence
Current Pharmaceutical Design Editorial
Current Medical Imaging Main Anti-tumor Angiogenesis Agents Isolated From Chinese Herbal Medicines
Mini-Reviews in Medicinal Chemistry The Pleiotropic Effects of PPARs on Vascular Cells and Angiogenesis: Implications for Tissue Engineering
Current Stem Cell Research & Therapy Targeting HOTAIR induces mitochondria related apoptosis and inhibits tumor growth in head and neck squamous cell carcinoma in vitro and in vivo.
Current Molecular Medicine Breast Cancer: Not Only a “Womans” Disease
Current Women`s Health Reviews Genetics of Cancer Susceptibility
Current Genomics Therapeutic Strategies for Targeting BRAF in Human Cancer
Reviews on Recent Clinical Trials Reality Check: Cancer Stem Cell Route to Cancer
Current Biotechnology How Similar are Human Mesenchymal Stem Cells Derived from Different Origins? A Review of Comparative Studies
Current Stem Cell Research & Therapy Targeting Ovarian Cancer-Initiating Cells
Anti-Cancer Agents in Medicinal Chemistry Histone Deacetylase Inhibition: A Differentiation Therapy for Cultured Primary Hepatocytes?
Current Enzyme Inhibition Eph/Ephrin Signalling and Function in Oncogenesis: Lessons from Embryonic Development
Current Cancer Drug Targets Garlic (<i>Allium sativum</i> L.): Its Chemistry, Nutritional Composition, Toxicity, and Anticancer Properties
Current Topics in Medicinal Chemistry A Molecular Link Between Diabetes and Breast Cancer: Therapeutic Potential of Repurposing Incretin-based Therapies for Breast Cancer
Current Cancer Drug Targets Effects of Novel Alkyl Pyridine Platinum Complexes on Apoptosis in Ishikawa Endometrial Cancer Cells
Medicinal Chemistry Effect of Curcumin on Pro-angiogenic Factors in the Xenograft Model of Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry Fibroblast Growth Factor-2, Bone Homeostasis and Fracture Repair
Current Pharmaceutical Design