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The -adrenergic receptors are linked to G proteins The -receptor has three known subtypes Beta-1 receptors primarily regulate myocardial tissue and affect the rate of contraction via impulse conduction Beta-2 receptors regulate smooth muscle tone and influence vascular and bronchiolar relaxation Beta-3 receptors are less well studied but are thought to primarily affect lypolysis and may have effects on cardiac inotropy (Greene Shepherd 2006) In the human heart beta (1)- and beta (2)AR are the most powerful physiologic mechanism to acutely increase cardiac performance Changes in betaAR play an important role in chronic heart failure (CHF) Thus due to increased sympathetic activity in CHF betaAR are chronically (over) stimulated and that results in beta (1) AR desensitization and alterations of down-stream mechanisms (Brodde OE 2006)
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Recombinant CHO-K1 cells stably overexpress human cholinergic receptor muscarinic 4 (M4) on the surface and contain high levels of G protein G i to couple with the receptor in downstream signaling pathways
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Recombinant CHO-K1 cells stably overexpress human opioid receptor delta 1 (OPRD1) on the surface and contain high levels of G protein G i to couple with the receptor in downstream signaling pathways
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The dihydroxy-leukotriene leukotriene B4 (LTB4) is a member of the G protein-coupled receptor (GPCR) family in a subfamily of GPCRs that includes receptors for chemokines and other chemotactic factors Recently a second lower affinity receptor for LTB4 (BLT2) has also been cloned with broader ligand specificity for various eicosanoids LTB4 stimulates neutrophil chemotaxis and secretion but may also affect immunomodulation contraction of certain smooth muscles via an indirect mechanism and activation of the nuclear transcription factor PPAR (peroxisome proliferation activated receptor alpha) Chemotaxis the principal effects of LTB4 and related dihydroxy-acids on leukocytes occurs via activation of BLT1 receptors
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Cluster of differentiation 40 CD40 is a costimulatory protein found on antigen presenting cells and is required for their activation The binding of CD154 (CD40L) on TH cells to CD40 activates antigen presenting cells and induces a variety of downstream effects
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Integrin alpha E (ITGAE) also known as CD103 (cluster of differentiation 103) is an integrin protein that in human ITGAE is expressed widely on intraepithelial lymphocyte (IEL) T cells (both T cells and T cells) and on some peripheral regulatory T cells (Tregs) It has also been reported on lamina propria T cells A subset of dendritic cells in the gut mucosa and mesenteric lymph nodes known as CD103 dendritic cells also expresses this marker
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V-domain Ig suppressor of T cell activation (VISTA) is a potent negative regulator of T-cell function that is expressed on hematopoietic cells VISTA levels are heightened within the tumor microenvironment in which its blockade can enhance antitumor immune responses in mice In humans blockade of the related programmed cell death 1 (PD-1) pathway has shown great potential in clinical immunotherapy trials
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BDCA-2 is a novel type II C-type lectin which shows 50 7% sequence identity at the amino acid level to its putative murine ortholog the murine dendritic cell associated C-type lectin 2 In addition to its antigen capturing function BDCA-2 can mediate potent inhibition of induction of IFN- / expression in PDCs Production of IFN- / in response to several different types of viruses bacteria CpG-DNA dsRNA and SLE serum is by far the most prominent feature of PDCs
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5-Hydroxytryptamine (5-HT also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals In the periphery 5-HT mediates gastrointestinal motility platelet aggregation and contraction of blood vessels Many functions of the central nervous system are influenced by 5-HT including sleep motor activity sensory perception arousal and appetite A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al 1994) 5-HT2B which couples to Gq/11 is expressed in embryonic and adult cardiovascular tissues gut and brain from the rat mouse and human species 5-HT2B receptors are responsible for many cardiovascular and central nervous system functions such as blood vessel contraction platelet shape changes neuronal sensitization to tactile stimuli and mediation of the hallucinogenic effects of phenylisopropylamin hallucinogens It has also been shown to be required for heart develo
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Recombinant CHO-K1 cells stably overexpress human adenosine A2A receptor (ADORA2A) on the surface and contain high levels of G protein G s to couple with the receptor in downstream signaling pathways
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The short form of D2 (D2S) and the long form (D2L) are two isoforms that contribute differentially to dopamine signaling in both prefrontal cortex and striatum The D2 dopamine receptor short form (D2s) has been shown to stimulate phospholipase D (PLD) activity independent of the activation of phospholipase C (PLC) activity in GH4 derived cells stably transfected with the D2s receptor Agonist activation of D2s has been shown to mediate the inhibition of growth in the same cell line
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The neuropeptide galanin elicits a range of biological effects by interacting with specific G-protein-coupled receptors Galanin receptors are seven-transmembrane proteins that have been shown to activate a variety of intracellular second-messenger pathways GALR1 inhibits adenylyl cyclase via a G protein of the Gi/Go family GALR1 is widely expressed in the brain spinal cord and peripheral sites including small intestine and heart
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The glucagon-like peptides include glucagon GLP-1 and GLP-2 exert diverse actions on nutrient intake gastrointestinal motility islet hormone secretion cell proliferation and apoptosis as well as nutrient absorptionand assimilation Glucagon-like peptide (GLP)-2 a product of the proglucagon gene is expressed in enteroendocrine cells of the small and large intestine and is trophic to the gastrointestinal mucosa GLP-2 also inhibits gastric acid secretion and emptying and up-regulates intestinal hexose transport GLP-2 acts via binding to a single G protein-coupled GLP-2 receptor (GLP-2R)
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