Abstract
Sphingosine 1-phosphate (S1P) is a bioactive lipid with diverse biological functions, including cell proliferation, differentiation, angiogenesis, chemotaxis, and migration. Many of the activities of S1P are mediated through five closely related G-protein-coupled receptors of the sphingosine-1-phosphate receptor family (S1PR) which play a crucial role in sphingolipid metabolism. Each of these receptors appears to be tissue specific and to have demonstrated roles in the regulation of cell proliferation and survival in various cancer types. Further analysis of the function that S1PRs serve in hematological malignancies offers a great potential for the discovery of novel and selective therapeutic agents targeting these receptors. This review focuses on the characterization of S1PRs and their roles in cancer development in various signaling pathways mediated through specific G coupled protein. In particular, pharmacological agents targeting these S1PRs will be discussed and their potential will be examined.
Keywords: Sphingosine-1-phosphate receptors (S1PR), Sphingosine-1-phosphate (S1P), leukemia, G-protein coupled receptors (GPCR), PKA, diacylglycerol, MAS, EDG, natural killer, cAMP=cyclic, COX-2, PDGF
Anti-Cancer Agents in Medicinal Chemistry
Title: Targeting Sphingosine-1-Phosphate Receptors in Cancer
Volume: 11 Issue: 9
Author(s): Rebecca J. Watters, Hong-Gang Wang, Shen-Shu Sung, Thomas P. Loughran and Xin Liu
Affiliation:
Keywords: Sphingosine-1-phosphate receptors (S1PR), Sphingosine-1-phosphate (S1P), leukemia, G-protein coupled receptors (GPCR), PKA, diacylglycerol, MAS, EDG, natural killer, cAMP=cyclic, COX-2, PDGF
Abstract: Sphingosine 1-phosphate (S1P) is a bioactive lipid with diverse biological functions, including cell proliferation, differentiation, angiogenesis, chemotaxis, and migration. Many of the activities of S1P are mediated through five closely related G-protein-coupled receptors of the sphingosine-1-phosphate receptor family (S1PR) which play a crucial role in sphingolipid metabolism. Each of these receptors appears to be tissue specific and to have demonstrated roles in the regulation of cell proliferation and survival in various cancer types. Further analysis of the function that S1PRs serve in hematological malignancies offers a great potential for the discovery of novel and selective therapeutic agents targeting these receptors. This review focuses on the characterization of S1PRs and their roles in cancer development in various signaling pathways mediated through specific G coupled protein. In particular, pharmacological agents targeting these S1PRs will be discussed and their potential will be examined.
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Cite this article as:
J. Watters Rebecca, Wang Hong-Gang, Sung Shen-Shu, P. Loughran Thomas and Liu Xin, Targeting Sphingosine-1-Phosphate Receptors in Cancer, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (9) . https://dx.doi.org/10.2174/187152011797655041
DOI https://dx.doi.org/10.2174/187152011797655041 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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