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Receptors for glucagon Gcgr GLP
2022-09-28

Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the Oxaliplatin australia for th
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Photoincorporation of pTFDBzox AP occurred
2022-09-27

Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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Although exhibited high inhibitory activity was found to be
2022-09-26

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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In the course of studies
2022-09-22

In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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In diseased blood vessels increased
2022-09-22

In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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Enzyme parameters obtained for GC
2022-09-22

Enzyme parameters obtained for GC-E variants can further be introduced in kinetic models of phototransduction using computational approaches. A similar approach has been successfully applied in the investigation of disease causing mutations of GCAP1 to simulate rod and cone photoresponses under dise
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Continuing studies of endocannabinoid ligands at GPR reveal
2022-09-22

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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Some years ago it has
2022-09-22

Some years ago, it has been described that CD45RA+ CD62L+ naïve CD4+ T AVE 0991 can be further differentiated into two distinct subpopulations by analysing their surface expression of CD31(Kimmig et al., 2002a; Kohler and Thiel, 2009; Kohler et al., 2005b). CD31+ thymicnaive CD4+ T cells are enriche
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The SLC A mutations identified in both
2022-09-21

The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran
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br Structures of human secretase
2022-09-21

Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a TPEN chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were speculate
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Type II diabetes is characterized by an
2022-09-21

Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty ISX 9 receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors and is primarily
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Recently the classical view of the compartmentalization of t
2022-09-21

Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic UM171 (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, the last two en
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Adipocytes play diverse roles in energy
2022-09-20

Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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In Kdm c germline and forebrain
2022-09-20

In Kdm5c germline and forebrain conditional knockout mice, RNA sequencing showed the upregulation of a large set of genes, suggesting that Kdm5c functions primarily as a transcriptional repressor [,]. While no changes in global H3K4me3 levels were observed in the knockout neurons, there were thousan
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The H autoreceptors distributed mainly in
2022-09-20

The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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