title: Molecular mechanisms of target recognition by lipid GPCRs: relevance for cancer.
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.
authors.affiliation: Department of Molecular Oncology, the Netherlands Cancer Institute, Amsterdam, The Netherlands.
authors.forename: M T M
authors.initials: MT
authors.lastname: van Jaarsveld
authors.affiliation: Department of Molecular Oncology, the Netherlands Cancer Institute, Amsterdam, The Netherlands.
authors.forename: J M
authors.initials: JM
authors.lastname: Houthuijzen
authors.affiliation: Department of Molecular Oncology, the Netherlands Cancer Institute, Amsterdam, The Netherlands.
authors.forename: E E
authors.initials: EE
authors.lastname: Voest
mesh_terms: D000818:Animals; D015777:Eicosanoids / Q000378:metabolism; D063388:Endocannabinoids / Q000502:physiology; D005227:Fatty Acids / Q000378:metabolism; D006801:Humans; D008055:Lipids / Q000502:physiology*; D008246:Lysophospholipids / Q000737:chemistry / Q000502:physiology; D009369:Neoplasms / Q000209:etiology / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled / Q000502:physiology*; D018077:Receptors, Leukotriene / Q000502:physiology; D049312:Receptors, Lysophospholipid / Q000502:physiology; D017482:Receptors, Thromboxane / Q000502:physiology; D015398:Signal Transduction
chemical_list: D015777:Eicosanoids; D063388:Endocannabinoids; D005227:Fatty Acids; D008055:Lipids; D008246:Lysophospholipids; D043562:Receptors, G-Protein-Coupled; D018077:Receptors, Leukotriene; D049312:Receptors, Lysophospholipid; D017482:Receptors, Thromboxane