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br Molecular mechanisms underpinning GSNOR function in the d
2022-07-27
Molecular mechanisms underpinning GSNOR1 function in the defence response Recently, Arabidopsis GSNOR1 has been shown to govern the extent of S-nitrosylation of two key regulatory proteins, Non-Expresser of Pathogenesis-Related Genes 1 (NPR1) and SA binding protein 3 (SABP3), which are integral t
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br Acknowledgments We thank Dr Kathleen Sullivan of Merck Re
2022-07-27
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 A 61603 hydrobromide expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, D
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GPR has been implicated in neuropathic and inflammatory
2022-07-27
GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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br Concluding Remarks Given the
2022-07-27
Concluding Remarks Given the increasing global incidence of metabolic disorders, new drugs that lower body weight and improve glucose tolerance are desperately needed. While we still have a long way to go, GPR55 might be an interesting target to explore, given its expression in numerous metaboli
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Among prostaglandins PG PGD remained the most elusive
2022-07-27
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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br Acknowledgments br Introduction Myelin
2022-07-27
Acknowledgments Introduction Myelin, one of the fundamental adaptations of vertebrates, is a multilamellar structure deriving from the spiral wrapping around the TC-E 5006 of the plasma membrane of myelin forming glia, oligodendrocytes in the central nervous system and Schwann cells (SC) in t
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br Materials and methods br Results br Discussion According
2022-07-27
Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 Brefeldin A has been identified within discrete regions of the nervo
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Even though for almost years
2022-07-27
Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi
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An alternative approach to improving pharmacokinetic profile
2022-07-27
An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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Recognition and Repair of DNA Damage DNA
2022-07-27
Recognition and Repair of DNA Damage DNA is a reactive molecule that is continually challenged by both endogenous and exogenous insults 1., 2.. Cellular metabolites and their byproducts, environmental toxins, and radiation alter the chemical structure of DNA, producing a wide spectrum of DNA damag
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br Introduction Glucose is the major carbon source in
2022-07-27
Introduction Glucose is the major carbon source in most organisms. Cancer 1-Oleoyl lysophosphatidic acid sodium salt australia in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic condit
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br Methods br Results br Discussion Previous work by the
2022-07-27
Methods Results Discussion Previous work by the Hirano group investigated the effect of GIP in murine atherosclerotic models and found infusion of GIP (1–42) by osmotic mini-pumps to decrease lesion size after 4 weeks in non-diabetic as well as in diabetic ApoE−/− mice [8], [9]. Mechanistic
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In the liver ghrelin has opposite effects
2022-07-27
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty osi sc 175 oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independent
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To improve the preferential GalR binding
2022-07-27
To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Posttraining memory facilitation by histamine infused into t
2022-07-26
Posttraining memory facilitation by histamine infused into the dorsal hippocampus was also observed in two more recently described and very important non-aversive forms of memory: object recognition (da Silveira, Furini, Benetti, Monteiro, & Izquierdo, 2013) and social recognition (Garrido Zinn et a
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