Results 71 to 80 of about 31,038,441 (242)

Differential activation mechanisms of lipid GPCRs by lysophosphatidic acid and sphingosine 1-phosphate

Nature Communications, 2022
Liu et al. report structures of human sphingosine 1-phosphate (S1P) receptor 1 (S1P1) in complex with Gi and S1P or the multiple sclerosis (MS) drug Siponimod, as well as human lysophosphatidic acid (LPA) receptor 1 (LPA1) in complex with Gi and LPA ...
Shian Liu, Navid Paknejad, Lan Zhu, Yasuyuki Kihara, Manisha Ray, Jerold Chun, Wei Liu, Richard K. Hite, Xin-Yun Huang   +8 more
doaj   +1 more source

The roles of bile acids and sphingosine-1-phosphate signaling in the hepatobiliary diseases

Journal of Lipid Research, 2016
Based on research carried out over the last decade, it has become increasingly evident that bile acids act not only as detergents, but also as important signaling molecules that exert various biological effects via activation of specific nuclear ...
Masayuki Nagahashi, Kizuki Yuza, Yuki Hirose, Masato Nakajima, Rajesh Ramanathan, Nitai C. Hait, Phillip B. Hylemon, Huiping Zhou, Kazuaki Takabe, Toshifumi Wakai   +9 more
doaj   +1 more source

An update on sphingosine-1-phosphate receptor 1 modulators [PDF]

Bioorganic & Medicinal Chemistry Letters, 2018
Sphingolipids represent an essential class of lipids found in all eukaryotes, and strongly influence cellular signal transduction. Autoimmune diseases like asthma and multiple sclerosis (MS) are mediated by the sphingosine-1-phosphate receptor 1 (S1P1) to express a variety of symptoms and disease patterns. Inspired by its natural substrate, an array of
Alexander Marciniak, Sara M. Camp, Joe G.N. Garcia, Robin Polt   +3 more
openaire   +2 more sources

Molecular recognition in the sphingosine 1-phosphate receptor family [PDF]

Journal of Molecular Graphics and Modelling, 2008
Computational modeling and its application in ligand screening and ligand receptor interaction studies play important roles in structure-based drug design. A series of sphingosine 1-phosphate (S1P) receptor ligands with varying potencies and receptor selectivities were docked into homology models of the S1P(1-5) receptors.
Truc-Chi T, Pham, James I, Fells, Daniel A, Osborne, E Jeffrey, North, Mor M, Naor, Abby L, Parrill   +5 more
openaire   +2 more sources

Structural basis for receptor selectivity and inverse agonism in S1P5 receptors

Nature Communications, 2022
S1P5 is a sphingosine-1-phosphate (S1P) receptor implicated in immune and neurodegenerative disorders. Here, authors report a crystal structure of the S1P5 receptor in complex with a selective inverse agonist, revealing an allosteric subpocket and ...
Elizaveta Lyapina, Egor Marin, Anastasiia Gusach, Philipp Orekhov, Andrey Gerasimov, Aleksandra Luginina, Daniil Vakhrameev, Margarita Ergasheva, Margarita Kovaleva, Georgii Khusainov, Polina Khorn, Mikhail Shevtsov, Kirill Kovalev, Sergey Bukhdruker, Ivan Okhrimenko, Petr Popov, Hao Hu, Uwe Weierstall, Wei Liu, Yunje Cho, Ivan Gushchin, Andrey Rogachev, Gleb Bourenkov, Sehan Park, Gisu Park, Hyo Jung Hyun, Jaehyun Park, Valentin Gordeliy, Valentin Borshchevskiy, Alexey Mishin, Vadim Cherezov   +30 more
doaj   +1 more source

Role of sphingosine-1-phosphate receptor 1 and downstream heme oxygenase-1 induction in alternative macrophage activation induced by apoptotic cells [PDF]

, 2010
Macrophages show a remarkable functional plasticity, which enables them to change their phenotype in response to environmental signals. They are key players during infection by initiating inflammation through the release of proinflammatory mediators ...
Weis, Nicole
core  

Sphingosine 1-phosphate signalling contributes to transforming growth factor-β1-induced myofibroblast differentiation in oral cancer [PDF]

PeerJ
The prognosis for patients with oral squamous cell carcinoma (OSCC) is poor and novel ways to manage the disease are required. The density of myofibroblastic cancer-associated fibroblasts (myoCAFs) within the OSCC stroma correlates with poor prognosis ...
Kathyleen Hui Lin Chong, Wee Lin Wong, Deron R. Herr, Wai-Leng Lee, Lee Fah Yap, Ian C. Paterson   +5 more
doaj   +2 more sources

Regulation of bile acid receptor activity

Liver Research, 2018
Many receptors can be activated by bile acids (BAs) and their derivatives. These include nuclear receptors farnesoid X receptor (FXR), pregnane X receptor (PXR), and vitamin D receptor (VDR), as well as membrane receptors Takeda G protein receptor 5 ...
Yu-Jui Yvonne Wan, Lili Sheng
doaj   +1 more source

Sphingosine-1-phosphate modulates PAR1-mediated human platelet activation in a concentration-dependent biphasic manner

Scientific Reports, 2021
Sphingosine 1-phosphate (S1P) is a bioactive signalling sphingolipid that is increased in diseases such as obesity and diabetes. S1P can modulate platelet function, however the direction of effect and S1P receptors (S1PRs) involved are controversial ...
Haonan Liu, Molly L. Jackson, Lucy J. Goudswaard, Samantha F. Moore, James L. Hutchinson, Ingeborg Hers   +5 more
doaj   +1 more source

Early‐stage health technology assessment of a curative gene therapy for multiple sclerosis

British Journal of Clinical Pharmacology, EarlyView.
Aims Multiple sclerosis (MS) is associated with significant early morbidity, reduced life expectancy and substantial healthcare and societal costs. The primary objective of this study is to assess the early cost‐effectiveness potential of a novel gene therapy, IMMUTOL, for MS compared with current high‐efficacy treatment sequences.
Attila Imre, Balázs Nagy, Rok Hren
wiley   +1 more source