Targeting Sphingosine-1-Phosphate Receptors in Cancer

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Targeting Sphingosine-1-Phosphate Receptors in Cancer

Anti-Cancer Agents in Medicinal Chemistry, 11(9): 810-817.

Author(s): Rebecca J. Watters, Hong-Gang Wang, Shen-Shu Sung, Thomas P. Loughran and Xin Liu.

Affiliation: Penn State Hershey Cancer Institute, Experimental Therapeutics -CH74, Room 4401, 500 University Drive, Hershey, PA 17033-0850.


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.


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.

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Article Details

Volume: 11
Issue Number: 9
First Page: 810
Last Page: 817
Page Count: 8
DOI: 10.2174/187152011797655041
Price: $58

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