Targeting the lipids LPA and S1P and their signalling pathways to inhibit tumour progression

Sphingosine-1-phosphate: an enigmatic signalling lipid

2003 • 2,022 citations

The Immune Modulator FTY720 Targets Sphingosine 1-Phosphate Receptors

2002 • 1,478 citations

Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors

1996 • 1,473 citations

The emerging role of lysophosphatidic acid in cancer

2003 • 1,086 citations

Autotaxin has lysophospholipase D activity leading to tumor cell growth and motility by lysophosphatidic acid production

2002 • 908 citations

Essential Role for Sphingosine Kinases in Neural and Vascular Development

2005 • 719 citations

Lysophosphatidic Acid as a Potential Biomarker for Ovarian and Other Gynecologic Cancers

1998 • 642 citations

SphK1 and SphK2, Sphingosine Kinase Isoenzymes with Opposing Functions in Sphingolipid Metabolism

2005 • 606 citations

Discovery and evaluation of inhibitors of human sphingosine kinase.

2003 • 586 citations

Identification, purification, and partial sequence analysis of autotaxin, a novel motility-stimulating protein.

1992 • 577 citations

LPA3-mediated lysophosphatidic acid signalling in embryo implantation and spacing

2005 • 541 citations

Autotaxin, a Secreted Lysophospholipase D, Is Essential for Blood Vessel Formation during Development

2006 • 524 citations

FTY720: Sphingosine 1-Phosphate Receptor-1 in the Control of Lymphocyte Egress and Endothelial Barrier Function

2004 • 462 citations

Autotaxin Stabilizes Blood Vessels and Is Required for Embryonic Vasculature by Producing Lysophosphatidic Acid

2006 • 451 citations

Validation of an anti-sphingosine-1-phosphate antibody as a potential therapeutic in reducing growth, invasion, and angiogenesis in multiple tumor lineages

2006 • 443 citations

The Sphingosine-1-phosphate Receptors S1P1, S1P2, and S1P3 Function Coordinately during Embryonic Angiogenesis

2004 • 402 citations

Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo

2006 • 400 citations

An oncogenic role of sphingosine kinase

2000 • 394 citations

Immunosuppressive and Anti-angiogenic Sphingosine 1-Phosphate Receptor-1 Agonists Induce Ubiquitinylation and Proteasomal Degradation of the Receptor

2007 • 394 citations

Ki16425, a Subtype-Selective Antagonist for EDG-Family Lysophosphatidic Acid Receptors

2003 • 392 citations

Sphingosine 1-Phosphate Induces Angiogenesis: Its Angiogenic Action and Signaling Mechanism in Human Umbilical Vein Endothelial Cells

1999 • 359 citations

Erythrocytes store and release sphingosine 1‐phosphate in blood

2007 • 355 citations

Characterization of an ovarian cancer activating factor in ascites from ovarian cancer patients.

1995 • 325 citations

Sphingosine Kinase-1 Expression Correlates With Poor Survival of Patients With Glioblastoma Multiforme: Roles of Sphingosine Kinase Isoforms in Growth of Glioblastoma Cell Lines

2005 • 321 citations

PKC-dependent Activation of Sphingosine Kinase 1 and Translocation to the Plasma Membrane

2002 • 293 citations

Antagonism of Sphingosine-1-Phosphate Receptors by FTY720 Inhibits Angiogenesis and Tumor Vascularization

2006 • 288 citations

Extracellular Export of Sphingosine Kinase-1 Enzyme

2002 • 281 citations

Sphingosine 1‐phosphate released from platelets during clotting accounts for the potent endothelial cell chemotactic activity of blood serum and provides a novel link between hemostasis and angiogenesis

2000 • 276 citations

Sphingosine 1-Phosphate Analogs as Receptor Antagonists

2004 • 267 citations

Effect of chemically well-defined sphingosine and its N-methyl derivatives on protein kinase C and src kinase activities

1989 • 259 citations

Antitumor Activity of Sphingosine Kinase Inhibitors

2006 • 239 citations

Autotaxin Is Overexpressed in Glioblastoma Multiforme and Contributes to Cell Motility of Glioblastoma by Converting Lysophosphatidylcholine TO Lysophosphatidic Acid

2006 • 238 citations

Lysophosphatidic acid and sphingosine 1-phosphate stimulate endothelial cell wound healing

2000 • 238 citations

Direct Quantitative Analysis of Lysophosphatidic Acid Molecular Species by Stable Isotope Dilution Electrospray Ionization Liquid Chromatography–Mass Spectrometry

2001 • 232 citations

Autotaxin hydrolyzes sphingosylphosphorylcholine to produce the regulator of migration, sphingosine-1-phosphate.

2003 • 223 citations

Estrogen transactivates EGFR via the sphingosine 1-phosphate receptor Edg-3: the role of sphingosine kinase-1

2006 • 220 citations

FTY720, A Novel Immunomodulator: Efficacy and Safety Results from the First Phase 2A Study in de novo Renal Transplantation

2004 • 216 citations

The type 1 lysophosphatidic acid receptor is a target for therapy in bone metastases

2006 • 205 citations

Intracellular Role for Sphingosine Kinase 1 in Intestinal Adenoma Cell Proliferation

2006 • 205 citations

I want a new drug: G-protein-coupled receptors in drug development

2006 • 201 citations

Requirement for sphingosine 1–phosphate receptor-1 in tumor angiogenesis demonstrated by in vivo RNA interference

2004 • 198 citations

Sphingosine Kinase-1 as a Chemotherapy Sensor in Prostate Adenocarcinoma Cell and Mouse Models

2005 • 198 citations

Lysophosphatidic acid synthesis and release

2001 • 198 citations

Lysophosphatidic Acid Is Constitutively Produced by Human Peritoneal Mesothelial Cells and Enhances Adhesion, Migration, and Invasion of Ovarian Cancer Cells

2006 • 196 citations

Autotaxin (NPP-2), a metastasis-enhancing motogen, is an angiogenic factor.

2001 • 194 citations

Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist

2002 • 191 citations

Inhibition of Autotaxin by Lysophosphatidic Acid and Sphingosine 1-Phosphate

2005 • 189 citations

Autotaxin (ATX), a potent tumor motogen, augments invasive and metastatic potential of ras-transformed cells

2000 • 188 citations

Requirement for sphingosine 1–phosphate receptor-1 in tumor angiogenesis demonstrated by in vivo RNA interference

2004 • 185 citations

The G Protein–Coupled Receptor S1P2 Regulates Rho/Rho Kinase Pathway to Inhibit Tumor Cell Migration

2005 • 179 citations

Malignant effusions contain lysophosphatidic acid (LPA)-like activity

1998 • 178 citations

Lysophosphatidic Acid (LPA) in Malignant Ascites Stimulates Motility of Human Pancreatic Cancer Cells through LPA1

2004 • 176 citations

Immunohistochemical Distribution of Sphingosine Kinase 1 in Normal and Tumor Lung Tissue

2005 • 176 citations

Lysophosphatidic acid as a phospholipid mediator: pathways of synthesis

1997 • 169 citations

Expression of autotaxin (NPP-2) is closely linked to invasiveness of breast cancer cells.

2002 • 163 citations

Synthesis and biological evaluation of γ-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists

2006 • 156 citations

Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors.

2001 • 153 citations

Carba Analogs of Cyclic Phosphatidic Acid Are Selective Inhibitors of Autotaxin and Cancer Cell Invasion and Metastasis

2006 • 152 citations

Identification of human renal cell carcinoma associated genes by suppression subtractive hybridization

2001 • 149 citations

The human lipid phosphate phosphatase-3 decreases the growth, survival, and tumorigenesis of ovarian cancer cells: validation of the lysophosphatidic acid signaling cascade as a target for therapy in ovarian cancer.

2003 • 142 citations

Aberrant expression of lysophosphatidic acid (LPA) receptors in human colorectal cancer

2004 • 140 citations

Sphingosine kinase activity counteracts ceramide-mediated cell death in human melanoma cells: role of Bcl-2 expression

2005 • 136 citations

High expression of sphingosine kinase 1 and S1P receptors in chemotherapy-resistant prostate cancer PC3 cells and their camptothecin-induced up-regulation

2006 • 134 citations

Brown recluse spider (Loxosceles reclusa) venom phospholipase D (PLD) generates lysophosphatidic acid (LPA)

2005 • 129 citations

Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study

2003 • 126 citations

LPA₂ receptor mediates mitogenic signals in human colon cancer cells

2005 • 126 citations

Autotaxin Expression in Non–Small-Cell Lung Cancer

1999 • 117 citations

Roles of sphingosine-1-phosphate (S1P) receptors in malignant behavior of glioma cells. Differential effects of S1P2 on cell migration and invasiveness

2007 • 116 citations

Over-expression of lysophosphatidic acid receptor-2 in human invasive ductal carcinoma

2004 • 110 citations

Extracellular release of newly synthesized sphingosine‐1‐phosphate by cerebellar granule cells and astrocytes

2005 • 109 citations

Expression, regulation and function of autotaxin in thyroid carcinomas

2004 • 109 citations

Induction of autotaxin by the Epstein-Barr virus promotes the growth and survival of Hodgkin lymphoma cells

2005 • 108 citations

Increased Production of Bioactive Lysophosphatidic Acid by Serum Lysophospholipase D in Human Pregnancy1

2002 • 105 citations

A pilot clinical/pharmacological study of the protein kinase C-specific inhibitor safingol alone and in combination with doxorubicin.

1997 • 103 citations

Synthesis, Structure−Activity Relationships, and Biological Evaluation of Fatty Alcohol Phosphates as Lysophosphatidic Acid Receptor Ligands, Activators of PPARγ, and Inhibitors of Autotaxin

2005 • 103 citations

FTY720 (fingolimod) in renal transplantation

2006 • 102 citations

Sphingosine 1-Phosphate Induces Membrane Ruffling and Increases Motility of Human Umbilical Vein Endothelial Cells via Vascular Endothelial Growth Factor Receptor and CrkII

2002 • 102 citations

Lysophosphatidic acid, a novel lipid growth factor for human thyroid cells: Over-expression of the high-affinity receptor edg4 in differentiated thyroid cancer

2001 • 98 citations

Abnormal serum lysophospholipids in multiple myeloma patients

1999 • 93 citations

α‐Substituted Phosphonate Analogues of Lysophosphatidic Acid (LPA) Selectively Inhibit Production and Action of LPA

2007 • 93 citations

Lysophosphatidic Acid-operated K+ Channels

2004 • 88 citations

Lysophosphatidic Acid Is a Major Regulator of Growth-Regulated Oncogene α in Ovarian Cancer

2006 • 87 citations

Sphingosine‐1‐phosphate modulates growth and adhesion of ovarian cancer cells

1999 • 87 citations

Identification of Residues Responsible for Ligand Recognition and Regioisomeric Selectivity of Lysophosphatidic Acid Receptors Expressed in Mammalian Cells

2005 • 86 citations

LPA-induced epithelial ovarian cancer (EOC) in vitro invasion and migration are mediated by VEGF receptor-2 (VEGF-R2)

2005 • 84 citations

Lipid Phosphate Phosphatases Regulate Lysophosphatidic Acid Production and Signaling in Platelets

2003 • 83 citations

S1P stimulates chemotactic migration and invasion in OVCAR3 ovarian cancer cells

2007 • 80 citations

Fatty Alcohol Phosphates are Subtype-Selective Agonists and Antagonists of Lysophosphatidic Acid Receptors

2003 • 80 citations

Sphingosine 1-Phosphate Receptor Expression Profile in Human Gastric Cancer Cells: Differential Regulation on the Migration and Proliferation1

2005 • 80 citations

Sphingosine 1-phosphate receptor expression profile and regulation of migration in human thyroid cancer cells

2006 • 79 citations

Biological functions of a novel lipid mediator, cyclic phosphatidic acid

2002 • 79 citations

S1P ₃ ‐mediated Akt activation and crosstalk with platelet‐derived growth factor receptor (PDGFR)

2003 • 75 citations

Phenoxodiol, an experimental anticancer drug, shows potent antiangiogenic properties in addition to its antitumour effects

2005 • 74 citations

Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor

2006 • 74 citations

Selective blockade of lysophosphatidic acid LPA₃receptors reduces murine renal ischemia-reperfusion injury

2003 • 73 citations

Homo- and hetero-dimerization of LPA/S1P receptors, OGR1 and GPR4

2006 • 72 citations

Follicular Fluid High Density Lipoprotein-associated Sphingosine 1-Phosphate Is a Novel Mediator of Ovarian Angiogenesis

2005 • 72 citations

Lysophosphatidic acid as an autocrine and paracrine mediator

2002 • 72 citations

Quantitative analysis of acyl-lysophosphatidic acid in plasma using negative ionization tandem mass spectrometry

2003 • 70 citations

The immunosuppressant FTY720 inhibits tumor angiogenesis via the sphingosine 1‐phosphate receptor 1

2007 • 69 citations

Involvement of Phospholipase D2 in Lysophosphatidate-induced Transactivation of Platelet-derived Growth Factor Receptor-β in Human Bronchial Epithelial Cells

2003 • 68 citations

Cyclic Phosphatidic Acid Is Produced by Autotaxin in Blood

2006 • 68 citations

Analysis of the mode of action of a novel immunosuppressant FTY720 in mice

1999 • 65 citations

Expression of autotaxin mRNA in human hepatocellular carcinoma.

1999 • 62 citations

Initial structure–activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist

2004 • 61 citations

FTY720/Cyclosporine Regimens in De Novo Renal Transplantation: A 1-Year Dose-Finding Study

2006 • 59 citations

Measurement of lysophospholipase D/autotaxin activity in human serum samples

2006 • 55 citations

FGFR4 GLY388 isotype suppresses motility of MDA-MB-231 breast cancer cells by EDG-2 gene repression

2005 • 54 citations

Existence of a bioactive lipid, cyclic phosphatidic acid, bound to human serum albumin

1999 • 54 citations

Lysophosphatidic receptor, LPA3, is positively and negatively regulated by progesterone and estrogen in the mouse uterus

2006 • 53 citations

Sphingosine kinase-1 – a potential therapeutic target in cancer

2006 • 52 citations

F-12509A, a New Sphingosine Kinase Inhibitor, Produced by a Discomycete.

2000 • 51 citations

Identifying Specific Conformations by Using a Carbohydrate Scaffold: Discovery of Subtype‐Selective LPA‐Receptor Agonists and an Antagonist

2004 • 47 citations

Sphingosine 1‐Phosphate Activates Erk‐1/‐2 by Transactivating Epidermal Growth Factor Receptor in Rat‐2 Cells

2000 • 46 citations

Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands

2005 • 46 citations

L-histidine inhibits production of lysophosphatidic acid by the tumor-associated cytokine, autotaxin

2005 • 44 citations

S-15183a and b, New Sphingosine Kinase Inhibitors, Produced by a Fungus.

2001 • 43 citations

Synthesis of Chiral (α,α-Difluoroalkyl)phosphonate Analogues of (Lyso)phosphatidic Acid via Hydrolytic Kinetic Resolution

2002 • 39 citations

Phase I trial of phenoxodiol delivered by continuous intravenous infusion in patients with solid cancer

2006 • 38 citations

Characterization of B-5354c, a New Sphingosine Kinase Inhibitor, Produced by a Marine Bacterium.

2000 • 37 citations

Differential expression of lysophosphatidic acid receptor‐2 in intestinal and diffuse type gastric cancer

2005 • 36 citations

Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors

2005 • 36 citations

Phosphonothioate and Fluoromethylene Phosphonate Analogues of Cyclic Phosphatidic Acid: Novel Antagonists of Lysophosphatidic Acid Receptors

2006 • 35 citations

Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists

2007 • 32 citations

Lysophospholipids transactivate HER2/neu (erbB-2) in human gastric cancer cells

2004 • 32 citations

Farnesyl phosphates are endogenous ligands of lysophosphatidic acid receptors: Inhibition of LPA GPCR and activation of PPARs

2006 • 31 citations

Phase I and pharmacokinetic study of weekly NV06 (Phenoxodiol™), a novel isoflav-3-ene, in patients with advanced cancer

2006 • 24 citations

Pharmacophore-Based Design of Sphingosine 1-phosphate-3 Receptor Antagonists That Include a 3,4-Dialkoxybenzophenone Scaffold

2007 • 23 citations

Expression of the endothelial cell differentiation gene 7 (EDG‐7), a lysophosphatidic acid receptor, in ovarian tumor

2005 • 17 citations

Synthesis and SAR studies of a novel class of S1P1 receptor antagonists

2007 • 14 citations

Immunotherapy for De Novo Renal Transplantation

2006 • 13 citations