Targeting sphingosine-1-phosphate receptors in cancer

Rebecca J. Watters, Hong-Gang Wang, Shen-shu Sung, Thomas P. Loughran, Xin Liu

Research output: Contribution to journalReview article

18 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)810-817
Number of pages8
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume11
Issue number9
StatePublished - Nov 1 2011

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Lysosphingolipid Receptors
Cell Proliferation
Sphingolipids
Hematologic Neoplasms
Chemotaxis
G-Protein-Coupled Receptors
Cell Differentiation
Neoplasms
Cell Survival
Pharmacology
Lipids
Proteins
sphingosine 1-phosphate
Therapeutics

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

Cite this

Watters, Rebecca J. ; Wang, Hong-Gang ; Sung, Shen-shu ; Loughran, Thomas P. ; Liu, Xin. / Targeting sphingosine-1-phosphate receptors in cancer. In: Anti-Cancer Agents in Medicinal Chemistry. 2011 ; Vol. 11, No. 9. pp. 810-817.
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Targeting sphingosine-1-phosphate receptors in cancer. / Watters, Rebecca J.; Wang, Hong-Gang; Sung, Shen-shu; Loughran, Thomas P.; Liu, Xin.

In: Anti-Cancer Agents in Medicinal Chemistry, Vol. 11, No. 9, 01.11.2011, p. 810-817.

Research output: Contribution to journalReview article

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AU - Wang, Hong-Gang

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AU - Loughran, Thomas P.

AU - Liu, Xin

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AB - 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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