Therapeutic potential of β-arrestin-and G protein-biased agonists
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …
Structure of S1PR2–heterotrimeric G13 signaling complex
Sphingosine-1-phosphate (S1P) regulates immune cell trafficking, angiogenesis, and
vascular function via its five receptors. Inherited mutations in S1P receptor 2 (S1PR2) occur …
vascular function via its five receptors. Inherited mutations in S1P receptor 2 (S1PR2) occur …
Aiming drug discovery at lysophosphatidic acid targets
G Tigyi - British journal of pharmacology, 2010 - Wiley Online Library
Lysophosphatidic acid (LPA, 1‐radyl‐2‐hydroxy‐sn‐glycero‐3‐phosphate) is the prototype
member of a family of lipid mediators and second messengers. LPA and its naturally …
member of a family of lipid mediators and second messengers. LPA and its naturally …
Role of the autotaxin–lysophosphatidate axis in cancer resistance to chemotherapy and radiotherapy
DN Brindley, FT Lin, GJ Tigyi - … et Biophysica Acta (BBA)-Molecular and Cell …, 2013 - Elsevier
High expression of autotaxin in cancers is often associated with increased tumor
progression, angiogenesis and metastasis. This is explained mainly since autotaxin …
progression, angiogenesis and metastasis. This is explained mainly since autotaxin …
Discovery of a novel orally active, selective LPA receptor type 1 antagonist, 4-(4-(2-isopropylphenyl)-4-((2-methoxy-4-methylphenyl) carbamoyl) piperidin-1-yl)-4 …
C Lescop, C Brotschi, JT Williams… - Journal of Medicinal …, 2024 - ACS Publications
Lysophosphatidic acid receptor 1 (LPAR1) antagonists show promise as potentially novel
antifibrotic treatments. In a human LPAR1 β-arrestin recruitment-based high-throughput …
antifibrotic treatments. In a human LPAR1 β-arrestin recruitment-based high-throughput …
Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad …
K Sobel, K Menyhart, N Killer, B Renault… - Journal of Biological …, 2013 - ASBMB
Synthetic sphingosine 1-phosphate receptor 1 modulators constitute a new class of drugs for
the treatment of autoimmune diseases. Sphingosine 1-phosphate (S1P) signaling, however …
the treatment of autoimmune diseases. Sphingosine 1-phosphate (S1P) signaling, however …
Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13
L Jenkins, J Brea, NJ Smith, BD Hudson… - Biochemical …, 2010 - portlandpress.com
The poorly characterized G-protein-coupled receptor GPR35 has been suggested as a
potential exploratory target for the treatment of both metabolic disorders and hypertension. It …
potential exploratory target for the treatment of both metabolic disorders and hypertension. It …
Selectivity and specificity of sphingosine-1-phosphate receptor ligands: caveats and critical thinking in characterizing receptor-mediated effects
S Salomone, C Waeber - Frontiers in pharmacology, 2011 - frontiersin.org
Receptors for sphingosine-1-phosphate (S1P) have been identified only recently. Their
medicinal chemistry is therefore still in its infancy, and few selective agonists or antagonists …
medicinal chemistry is therefore still in its infancy, and few selective agonists or antagonists …
Sphingosine-1-phosphate induces airway smooth muscle cell proliferation, migration, and contraction by modulating Hippo signaling effector YAP
L Liu, C Zhai, Y Pan, Y Zhu, W Shi… - … of Physiology-Lung …, 2018 - journals.physiology.org
Sphingosine-1-phosphate (S1P), a bioactive lipid, has been shown to be elevated in the
airways of individuals with asthma and modulates the airway smooth muscle cell (ASMC) …
airways of individuals with asthma and modulates the airway smooth muscle cell (ASMC) …
Druggable lipid GPCRs: past, present, and prospects
H Mizuno, Y Kihara - Druggable Lipid Signaling Pathways, 2020 - Springer
G protein-coupled receptors (GPCRs) have seven transmembrane spanning domains and
comprise the largest superfamily with~ 800 receptors in humans. GPCRs are attractive …
comprise the largest superfamily with~ 800 receptors in humans. GPCRs are attractive …