摘要
沙利度胺是具有有趣治疗特性的药物,但也有严重的副作用,需要仔细和监测使用。潜在的免疫调节,抗炎,抗血管生成和镇静作用使沙利度胺成为治疗多种疾病如多发性骨髓瘤的良好候选药物。通过增加TNFα-mRNA的降解,沙利度胺通过脂多糖或由有丝分裂刺激诱导的T淋巴细胞刺激的单核细胞和巨噬细胞减少TNFα的产生。降低的TNFα水平通过阻止NF-kB的激活和减少参与细胞增殖,炎症,血管发生和保护细胞凋亡的蛋白质,特别是IL-6的合成来改变细胞内转导的机制。此外,沙利度胺通过下调其表达影响VEGF水平。如今,新的更安全和毒性较小的药物,沙利度胺的类似物正在出现,可用于更有针对性地治疗多发性骨髓瘤和其他几种疾病,如克罗恩病,类风湿性关节炎,结节病,红斑性红斑,移植物抗宿主病。
关键词: 沙利度胺,血管发生,TNF-α,IL-6,VEGF,沙利度胺类似物
Current Medicinal Chemistry
Title:A Mini-Review on Thalidomide: Chemistry, Mechanisms of Action, Therapeutic Potential and Anti-Angiogenic Properties in Multiple Myeloma
Volume: 24 Issue: 25
关键词: 沙利度胺,血管发生,TNF-α,IL-6,VEGF,沙利度胺类似物
摘要: Thalidomide is a drug with interesting therapeutic properties but also with severe side effects which require a careful and monitored use. Potential immunomodulatory, antiinflammatory, anti-angiogenic and sedative properties make thalidomide a good candidate for the treatment of several diseases such as multiple myeloma. Through an increase in the degradation of TNFα-mRNA, thalidomide reduces the production of TNFα by monocytes and macrophages stimulated by lipopolysaccharide or by T lymphocytes induced by mitogenic stimuli. The decreased level of TNFα alters the mechanisms of intracellular transduction by preventing the activation of NF-kB and by decreasing the synthesis of proteins, in particular IL-6, involved in cell proliferation, inflammation, angiogenesis and protection from apoptosis. Furthermore, thalidomide affects VEGF levels by down-regulating its expression. Nowadays, new safer and less toxic drugs, analogs of thalidomide, are emerging as beneficial for a more targeted treatment of multiple myeloma and several other diseases such as Crohn's disease, rheumatoid arthritis, sarcoidosis, erythema nodosum leprosum, graft-versus-host disease.
Export Options
About this article
Cite this article as:
A Mini-Review on Thalidomide: Chemistry, Mechanisms of Action, Therapeutic Potential and Anti-Angiogenic Properties in Multiple Myeloma, Current Medicinal Chemistry 2017; 24 (25) . https://dx.doi.org/10.2174/0929867324666170601074646
DOI https://dx.doi.org/10.2174/0929867324666170601074646 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
Quinone Bioreductive Prodrugs as Delivery Agents
Current Drug Delivery An Evidence-Based Review of the Mechanism of Action, Efficacy, and Safety of Biologic Therapies in the Treatment of Psoriasis and Psoriatic Arthritis
Current Medicinal Chemistry Recent Insights into the Role of Prostanoids in Atherosclerotic Vascular Disease
Current Vascular Pharmacology Editorial (Thematic Issue: The Urgent Need to Reform the Present System of Medicines’ Regulation)
Reviews on Recent Clinical Trials A Summary of Electrospun Nanofibers as Drug Delivery System: Drugs Loaded and Biopolymers Used as Matrices
Current Drug Delivery Recent Advances in Small Molecule Prodrugs for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry COPD: Optimal Current Treatment Strategies and Promising New Therapeutic Modalities
Current Respiratory Medicine Reviews Targeting Cytokines, Chemokines and Adhesion Molecules in Rheumatoid Arthritis
Current Rheumatology Reviews Modulation of Regulatory T Cells in Health and Disease: Role of Toll-Like Receptors
Inflammation & Allergy - Drug Targets (Discontinued) Osmotically Regulated Flow of Flurbiprofen through In Situ Formed Asymmetric Membrane Capsule
Current Drug Delivery Renal & Ocular Targets for Therapy in Wegeners Granulomatosis
Inflammation & Allergy - Drug Targets (Discontinued) Editorial [ Targeting G Protein-Coupled 7TM Receptors in Inflammation Guest Editor: Dr. Trond Ulven ]
Current Topics in Medicinal Chemistry Neopterin as a Marker for Immune System Activation
Current Drug Metabolism Pentraxins and Atherosclerosis: The Role of PTX3
Current Pharmaceutical Design Methotrexate in the Treatment of Psoriasis and Rheumatoid Arthritis: Mechanistic Insights, Current Issues and Novel Delivery Approaches
Current Pharmaceutical Design Advances in Therapy for Psoriasis: An Overview of Infliximab, Etanercept, Efalizumab, Alefacept, Adalimumab, Tazarotene, and Pimecrolimus
Current Pharmaceutical Design Editorial (Hot Topic:Rheumatoid Arthritis: Current Advances in Pathogenesis, Diagnosis and Therapy)
Current Topics in Medicinal Chemistry Leukocyte Function-Associated Antigen-1: Structure, Function and Application Prospects
Protein & Peptide Letters Asymmetric Dimethylarginine: Clinical Significance and Novel Therapeutic Approaches
Current Medicinal Chemistry Part-Time α-Secretases: The Functional Biology of ADAM 9, 10 and 17
Current Alzheimer Research