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GLP is released in response
2021-11-29

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Amiloride HCl dihydrate receptor 4 (FFA4/GPR120) as a potential 7TM recepto
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In the present studies we
2021-11-29

In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 Bestatin hydrochloride and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS)
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Potential platelet related mechanisms that might explain
2021-11-29

Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu
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Three additional Type I CDK and
2021-11-29

Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an I
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br Experimental br Results and
2021-11-29

Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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The finding that GPR acts as a receptor for
2021-11-29

The finding that GPR35 acts as a receptor for 2-acyl LPA is noteworthy, because P2Y5, which has homology with GPR35 (29%), has recently been shown to act as a receptor for 2-acyl LPA [14]. LPA3 is also a specific receptor for 2-acyl LPA [15]. It is also worth noting that GPR55, which has homology w
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In the present study five
2021-11-26

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Because AM had limited efficacy
2021-11-26

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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Herein we report the discovery
2021-11-26

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Aminoallyl-dCTP - Cy3 So what makes a FFAR agonist different
2021-11-26

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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br PEPCK This enzyme decarboxylates and then
2021-11-26

PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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Accordingly and in animal models a
2021-11-26

Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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The effect of combined A and PD
2021-11-26

The effect of combined A-192621 and PD 155080 treatment on the Alrestatin during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min, and wa
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Surface enhanced Raman spectroscopy SERS is one
2021-11-26

Surface-enhanced Raman spectroscopy (SERS) is one of the most powerful and ultra-sensitive analytical tools, which has been widely applied to food security analysis and many other fields (Craig, Franca, & Irudayaraj, 2013; Gukowsky, Xie, Gao, Qu, & He, 2018; Qi et al., 2013; Zhang et al., 2015). For
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OS has a key role in
2021-11-26

OS has a key role in the pathogenesis of micro- and macrovascular diabetic complications [3]. There is now convincing evidence that the enzymes that generate ROS and gasotransmitters, such as nitric oxide (NO) and CO, are redox regulated at both the transcription and activity levels, and are also im
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