摘要
鞘脂(SL)不仅是细胞膜中的结构脂质,而且是不同细胞过程的关键调节器这一事实已得到公认。1-磷酸鞘氨醇(S1P)是其的一个组成部分,尤其是在细胞迁移、血管生成和细胞增殖过程中,能够发挥不同的细胞内和细胞外的作用。当S1P转运出细胞,它结合S1P特异性G蛋白偶联受体,主要参与免疫调节、血管和神经系统。这些结果解释了由S1P受体激活引起的功能多样性。S1P水平的失调与一些疾病相关,如自身免疫性疾病和癌症。因此,正确的调制这些受体对新治疗策略的发展是有意义的。沿着这个思维模式,非选择性的S1P受体激动剂芬戈莫德(FTY720)最近已经商业化,用于治疗多发性硬化症并且几个相关的S1P受体调节剂治疗正在进行临床试验。然而,尽管这一领域有所进展,但是S1P受体的生物学功能仍不清楚。因此,为了更好地了解这些受体的功能,利用新的选择性S1P受体激动剂和拮抗剂的药理学工具研究正在开发中。
关键词: 1-磷酸鞘氨醇,受体,调制,芬戈莫德,多发性硬化症。
Current Medicinal Chemistry
Title:Therapeutic Potential of the Modulation of Sphingosine-1-Phosphate Receptors
Volume: 23 Issue: 3
Author(s): Antonio Delgado and Miriam Martínez-Cartro
Affiliation:
关键词: 1-磷酸鞘氨醇,受体,调制,芬戈莫德,多发性硬化症。
摘要: It is accepted that sphingolipids (SL) are not only structural lipids in cellular membranes, but also key regulators of different cell process. Sphingosine-1-phosphate (S1P) is a member of this family involved, inter alia, in cell migration, angiogenesis and cell proliferation processes, being able to play different intracellular and extracellular roles. When S1P is transported out of the cell, it binds S1P specific G protein-coupled receptors, which are mainly involved in the regulation of the immune, vascular and nervous systems. These effects account for the vast diversity of functions that arise from the activation of S1P receptors. Deregulation of S1P levels is correlated with several pathologies, such as autoimmune disorders and cancer. Consequently, the correct modulation of these receptors represents a valuable approach for the development of new therapeutic strategies. Along this line, the non-selective S1P receptor agonist fingolimod (FTY720) has been commercialized recently for the treatment of multiple sclerosis and several related S1P receptor modulators are ongoing clinical trials. However, despite the progress in this field, the biological functions of S1P receptors are not still well elucidated. For this reason, several studies are being developed in order to better understand the functions of these receptors, making use of new selective S1P receptor agonists and antagonists as pharmacological tools.
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Cite this article as:
Antonio Delgado and Miriam Martínez-Cartro , Therapeutic Potential of the Modulation of Sphingosine-1-Phosphate Receptors, Current Medicinal Chemistry 2016; 23 (3) . https://dx.doi.org/10.2174/0929867323666151207111509
DOI https://dx.doi.org/10.2174/0929867323666151207111509 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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