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]
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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Objective: Glucagon-like peptide-1 and glucagon receptor (GLP-1R/GCGR) co-agonism can maximise weight loss and improve glycaemic control in type 2 diabetes and obesity.
Phil Pickford +15 more
doaj +1 more source
G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
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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β-arrestin 2 quenches TLR signaling to facilitate the immune evasion of EPEC
The protein translocated intimin receptor (Tir) from enteropathogenic Escherichia coli shares sequence similarity with the host cellular immunoreceptor tyrosine-based inhibition motifs (ITIMs).
Zijuan Chen +11 more
doaj +1 more source
Pharmacogenetics of analgesic drugs [PDF]
• Individual variability in pain perception and differences in the efficacy of analgesic drugs are complex phenomena and are partly genetically predetermined.
Branford, R +4 more
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Galanin receptor 2 modifies neuropeptide Y Y1 receptor internalization and β-Arrestin recruitment [PDF]
We have recently described a Galanin receptor 2(GALR2) and Neuropeptide Y Y1 receptor(NPYY1R) interaction at behavioural, cellular and receptor levels through GALR2/NPYY1R heterodimers.
Borroto-Escuela, Dasiel +8 more
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CXCL12 and [N33A]CXCL12 in 5637 and HeLa cells: regulating HER1 phosphorylation via calmodulin/calcineurin. [PDF]
In the human neoplastic cell lines 5637 and HeLa, recombinant CXCL12 elicited, as expected, downstream signals via both G-protein-dependent and β-arrestin-dependent pathways responsible for inducing a rapid and a late wave, respectively, of ERK1/2 ...
Antonella Rigo +6 more
doaj +1 more source
A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. [PDF]
It is well known that the ω-3 fatty acids (ω-3-FAs; also known as n-3 fatty acids) can exert potent anti-inflammatory effects. Commonly consumed as fish products, dietary supplements and pharmaceuticals, ω-3-FAs have a number of health benefits ascribed ...
Akiyama, Taro E +20 more
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Novel mechanisms of G-protein-coupled receptors functions: AT1 angiotensin receptor acts as a signaling hub and focal point of receptor cross-talk [PDF]
AT1 angiotensin receptor (AT1R), a prototypical G protein-coupled receptor (GPCR), is the main receptor, which mediates the effects of the renin-angiotensin system (RAS).
Balla, András +3 more
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Heat Shock Protein 20 (HSP20) is a novel substrate for Protein Kinase D1 (PKD1) [PDF]
Heat shock protein 20 (HSP20) has cardioprotective qualities, which are triggered by PKA phosphorylation. PKD1 is also a binding partner for HSP20, and this prompted us to investigate whether the chaperone was a substrate for PKD1.
Baillie, George, Sin, Yuan Yan
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