scholarly journals The human G protein‐coupled ATP receptor P2Y 11 is a target for anti‐inflammatory strategies

2021 ◽  
Author(s):  
Georg Gruenbacher ◽  
Hubert Gander ◽  
Gabriele Dobler ◽  
Andrea Rahm ◽  
Dominik Klaver ◽  
...  
Keyword(s):  
G Protein ◽  
Anti Inflammatory ◽  
G Protein Coupled

Small Molecules that Mimic Components of Bioactive Protein Surfaces

2004 ◽  
Vol 57 (9) ◽  
pp. 855 ◽  
Author(s):  
David P. Fairlie
Keyword(s):  
Amino Acids ◽  
Antiviral Activity ◽  
Small Molecules ◽  
G Protein ◽  
Selective Inhibition ◽  
Structural Components ◽  
Protein Surfaces ◽  
Biological Responses ◽  
Anti Inflammatory ◽  
G Protein Coupled

Small molecules designed to mimic specific structural components of a protein (peptide strands, sheets, turns, helices, or amino acids) can be expected to display agonist or antagonist biological responses by virtue of interacting with the same receptors that recognize the protein. Here we describe some minimalist approaches to structural mimetics of amino acids and of strand, turn, or helix segments of proteins. The designed molecules show potent and selective inhibition of protease, transferase, and phospholipase enzymes, or antagonism of G-protein coupled or transcriptional receptors, and have potent anti-tumour, anti-inflammatory, or antiviral activity.

scholarly journals The Controversial C5a Receptor C5aR2: Its Role in Health and Disease

2017 ◽  
Vol 2017 ◽  
pp. 1-16 ◽  
Author(s):  
Ting Zhang ◽  
Malgorzata A. Garstka ◽  
Ke Li
Keyword(s):  
Animal Models ◽  
G Protein ◽  
Cellular Localization ◽  
G Protein Coupled Receptor ◽  
C5a Receptor ◽  
Intracellular Signals ◽  
Health And Disease ◽  
Anti Inflammatory ◽  
G Protein Coupled

After the discovery of the C5a receptor C5aR1, C5aR2 is the second receptor found to bind C5a and its des-arginine form. As a heptahelical G protein-coupled receptor but devoid of the intracellular Gα signal, C5aR2 is special and confusing. Ramifications and controversies about C5aR2 are under debate since its identification, from putative ligands and cellular localization to intracellular signals and pathological roles in inflammation and immunity. The ruleless and even conflicting pro- or anti-inflammatory role of C5aR2 in animal models of diverse diseases makes one bewildered. This review summarizes reports on C5aR2, tries to clear up available evidence on these four controversial aspects, and delineates C5aR2 function(s). It also summarizes available toolboxes for C5aR2 study.

Lysophosphatidylinositol, an Endogenous Ligand for G Protein-Coupled Receptor 55, Has Anti-inflammatory Effects in Cultured Microglia

Inflammation ◽  
2020 ◽  
Vol 43 (5) ◽  
pp. 1971-1987
Author(s):  
Tomoki Minamihata ◽  
Katsura Takano ◽  
Mitsuaki Moriyama ◽  
Yoichi Nakamura
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Endogenous Ligand ◽  
Anti Inflammatory ◽  
G Protein Coupled

G protein-coupled estrogen receptor is involved in the anti-inflammatory effects of genistein in microglia

Phytomedicine ◽  
2018 ◽  
Vol 43 ◽  
pp. 11-20 ◽  
Author(s):  
Zhong-Rui Du ◽  
Xiao-Qing Feng ◽  
Na Li ◽  
Jiang-Xue Qu ◽  
Lu Feng ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Anti Inflammatory ◽  
G Protein Coupled

scholarly journals Lipid Mediator n-3 Docosapentaenoic Acid-Derived Protectin D1­(PD1n-3DPA) Enhances Synaptic Inhibition of Hippocampal Principal Neurons by Interaction with a G-Protein Coupled Receptor

2021 ◽  
Author(s):  
Apostolos Mikroulis ◽  
Marco Ledri ◽  
Gabriele Ruffolo ◽  
Eleonora Palma ◽  
Günther Sperk ◽  
...  
Keyword(s):  
G Protein ◽  
Neuronal Activity ◽  
Pyramidal Neurons ◽  
Hippocampal Slices ◽  
Docosapentaenoic Acid ◽  
Inhibitory Synapses ◽  
Lipid Mediator ◽  
Synaptic Inputs ◽  
Anti Inflammatory ◽  
G Protein Coupled

Abstract Epilepsy is a severe neurological disease manifested by spontaneous recurrent seizures due to abnormal hyper-synchronisation of neuronal activity. Epilepsy affects about 1% of the population and up to 40% of patients experience seizures that are resistant to currently available drugs, thus highlighting an urgent need for novel treatments. In this regard, anti-inflammatory drugs emerged as potential therapeutic candidates. In particular, specific molecules apt to resolve the neuroinflammatory response occurring in acquired epilepsies have been proven to counteract seizures in experimental models, and in humans. One candidate investigational molecule has been recently identified as the lipid mediator n-3 docosapentaenoic acid-derived protectin D1(PD1 n-3DPA ) which significantly reduced seizures, cell loss and cognitive deficit in a mouse model of acquired epilepsy. However, the mechanisms that mediate PD1 n-3DPA effect remain elusive. We here addressed whether PD1 n-3DPA has direct effects on neuronal activity independent on its anti-inflammatory action. We incubated therefore hippocampal slices with PD1 n-3DPA and investigated its effect on excitatory and inhibitory synaptic inputs to the CA1 pyramidal neurons. We demonstrate that inhibitory drive onto the perisomatic region of the pyramidal neurons is increased by PD1 n-3DPA , and this effect is mediated by pertussis toxin-sensitive G-protein coupled receptors. Our data indicate that PD1 n-3DPA acts directly on inhibitory transmission, most likely at presynaptic site of inhibitory synapses as also supported by oocyte and immunohistochemical experiments. Thus, in addition to its anti-inflammatory effects, PD1 n-3DPA anti-seizure and neuroprotective effects may be mediated by its direct action on neuronal excitability by modulating their synaptic inputs.

G protein-coupled receptor 39 plays an anti-inflammatory role by enhancing IL-10 production from macrophages under inflammatory conditions

2018 ◽  
Vol 834 ◽  
pp. 240-245 ◽  
Author(s):  
Satoshi Muneoka ◽  
Megumi Goto ◽  
Kumiko Kadoshima-Yamaoka ◽  
Reiko Kamei ◽  
Maki Terakawa ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Inflammatory Conditions ◽  
Anti Inflammatory ◽  
G Protein Coupled

scholarly journals G protein-coupled estrogen receptor mediates anti-inflammatory action in Crohn’s disease

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Damian Jacenik ◽  
Marta Zielińska ◽  
Anna Mokrowiecka ◽  
Sylwia Michlewska ◽  
Ewa Małecka-Panas ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Crohn’S Disease ◽  
Crohn's Disease ◽  
G Protein ◽  
Anti Inflammatory ◽  
G Protein Coupled ◽  
Inflammatory Action

scholarly journals AMP010014A09 in Sus Scrofa Encodes an Analog of G Protein-Coupled Receptor 109A, Which Mediates the Anti-Inflammatory Effects of Beta-Hydroxybutyric Acid

2017 ◽  
Vol 42 (4) ◽  
pp. 1420-1430 ◽  
Author(s):  
Guangxin Chen ◽  
Shoupeng Fu ◽  
Wenqian Feng ◽  
Bingxu Huang ◽  
Shiyao Xu ◽  
...  
Keyword(s):  
G Protein ◽  
Inflammatory Cytokines ◽  
Sus Scrofa ◽  
Hydroxybutyric Acid ◽  
G Protein Coupled Receptor ◽  
Anti Inflammatory ◽  
High Level ◽  
G Protein Coupled ◽  
Camp Levels ◽  
Pro Inflammatory Cytokines

Background: Hydroxy-carboxylic acid receptor 2 (HCA2, also called GPR109A) belongs to the G protein-coupled receptor (GPCR) family and is found in humans, rats, mice, hamsters and guinea pigs, but there are almost no reports of this protein in other species. In this investigation, we speculated that AMP010014A09 (AMP+) is a homologue of GPR109A in swine. Methods: To test this hypothesis, the following experiments were designed: monocytes isolated from the peripheral blood of swine were treated with LPS after pretreating with or without β-hydroxybutyric acid (BHBA), and the levels of pro-inflammatory cytokines and inflammatory proteins were assessed. cAMP levels induced by Forskolin in swine testicular (ST) and IPEC-J2 cells were detected with or without BHBA treatment and following silencing or stable transfection of the AMP+ gene. Results: AMP+ in swine exhibited a high level of homology with HM74A in humans and PUMA-G in mice. BHBA inhibited the LPS-induced secretion of the pro-inflammatory cytokines TNF-α, IL-6 and IL-1β and the inflammatory protein COX-2 in monocytes of swine. BHBA suppressed the Forskolin-induced cAMP level increase in ST cells, but failed to inhibit the accumulation of cAMP after the AMP+ gene was silenced with shRNA by transfecting cells with the pGPU6-GFP-Neo-AMP+-sus-392 plasmid. BHBA had no effect on cAMP levels in IPEC-J2 cells, but significantly inhibited the increase in cAMP induced by Forskolin treatment following transfection of the AMP+ gene into IPEC-J2 cells by a lentivirus vector. Conclusion: Our results indicated that AMP+ encodes a G protein-coupled receptor in Sus scrofa that inhibits cAMP levels and mediates anti-inflammatory effects in swine monocytes.

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