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Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer

Oncogene volume 35, pages 4021–4035 (2016)Cite this article

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Abstract

Over the past decade the importance of lipids for cancer cell metabolism and cancer-related processes such as proliferation, metastasis and chemotherapy resistance has become more apparent. The mechanisms by which lipid signals are transduced are poorly understood, but frequently involve G-protein Coupled Receptors (GPCRs), which can be explored as druggable targets. Here, we discuss how GPCRs recognize four classes of cancer-relevant lipids (lysophospholipids, phospholipids, fatty acids and eicosanoids). We compare the ligand-binding properties of >50 lipid receptors, we examine how their dysregulation contributes to tumorigenesis and how they may be therapeutically exploited.

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Acknowledgements

We thank Dr Perrakis and Dr Moolenaar for helpful discussions. The study was funded by Dutch Cancer Society grants UU2012-5712 and UU2009-4534.

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  1. M T M van Jaarsveld

    Present address: 1Current address: Max Planck Institute for Molecular Genetics, Otto Warburg Laboratory, Berlin, Germany.,

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  1. Department of Molecular Oncology, the Netherlands Cancer Institute, Amsterdam, The Netherlands

    M T M van Jaarsveld, J M Houthuijzen & E E Voest

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van Jaarsveld, M., Houthuijzen, J. & Voest, E. Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer. Oncogene 35, 4021–4035 (2016). https://doi.org/10.1038/onc.2015.467

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