What doesn't kill you makes you stranger: Dipeptidyl peptidase-4 (CD26) proteolysis differentially modulates the activity of many peptide hormones and cytokines generating novel cryptic bioactive ligands [PDF]
, 2019 Dipeptidyl peptidase 4 (DPP4) is an exopeptidase found either on cell surfaces where it is highly regulated in terms of its expression and surface availability (CD26) or in a free/circulating soluble constitutively available and intrinsically active form.
Aguilar-Pérez, Alexandra +13 more
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G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease [PDF]
, 2015 G protein-coupled receptor 35 (GPR35) is an orphan receptor, discovered in 1998, that has garnered interest as a potential therapeutic target through its association with a range of diseases.
Amanda E Mackenzie +4 more
core +3 more sources
β-Arrestin-dependent deactivation of mouse melanopsin.
PLoS ONE, 2014 In mammals, the expression of the unusual visual pigment, melanopsin, is restricted to a small subset of intrinsically photosensitive retinal ganglion cells (ipRGCs), whose signaling regulate numerous non-visual functions including sleep, circadian ...
Evan G Cameron, Phyllis R Robinson
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G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
, 2017 It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
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Surfactant protein-A modulates LPS-induced TLR4 localization and signaling via β-arrestin 2. [PDF]
PLoS ONE, 2013 The soluble C-type lectin surfactant protein (SP)-A mediates lung immune responses partially via its direct effects on alveolar macrophages (AM), the main resident leukocytes exposed to antigens. SP-A modulates the AM threshold of lipopolysaccharide (LPS)
Vicky Sender, Linda Lang, Cordula Stamme
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Differential Involvement of ACKR3 C-Tail in β-Arrestin Recruitment, Trafficking and Internalization
Cells, 2021 Background: The atypical chemokine receptor 3 (ACKR3) belongs to the superfamily of G protein-coupled receptors (GPCRs). Unlike classical GPCRs, this receptor does not activate G proteins in most cell types but recruits β-arrestins upon activation. ACKR3
Aurélien Zarca +9 more
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Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]
, 2016 This Letter was supported by the Biotechnology and Biological Sciences Research Council (BBSRC) and the Scottish Universities Life Sciences Alliance (SULSA) in 2011Peer ...
Abdelrahman, Mostafa Hamed +4 more
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Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands [PDF]
, 2015 Short chain fatty acids (SCFAs) are produced in the gut by bacterial fermentation of poorly digested carbohydrates. A key mediator of their actions is the G protein-coupled Free Fatty Acid 2 (FFA2) receptor and this has been suggested as a therapeutic ...
Hansen, Anders Højgaard +6 more
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β-Arrestin1 and 2 differentially regulate PACAP-induced PAC1 receptor signaling and trafficking. [PDF]
PLoS ONE, 2018 A pituitary adenylate cyclase-activating polypeptide (PACAP)-specific receptor, PAC1R, is coupled with multiple signal transduction pathways including stimulation of adenylate cyclase, phospholipase C and extracellular-signal regulated kinase (ERK)1/2 ...
Yusuke Shintani +8 more
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The Effects of Apelin and Elabela Ligands on Apelin Receptor Distinct Signaling Profiles
Frontiers in Pharmacology, 2021 Apelin and Elabela are endogenous peptide ligands for Apelin receptor (APJ), a widely expressed G protein-coupled receptor. They constitute a spatiotemporal dual ligand system to control APJ signal transduction and function.
Yunlu Jiang +11 more
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