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The first rationally designed dual mPGES LO inhibitor was
2023-08-26
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic nitric oxide synthase inhibitor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivati
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Aurora A or B selective and
2023-08-26
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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Having demonstrated that Gq coupled mGluR a was necessary fo
2023-08-26
Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in
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The approach of enzymatically converting an analyte and dete
2023-08-26
The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl
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br APJ expression in metabolic diseases Under physiological
2023-08-26
APJ expression in metabolic diseases Under physiological conditions, APJ is present in humans as well as in mouse tissues with high metabolic activity such as muscle and adipose tissue but not in the liver. Moreover, the presence and regulation of APJ in established adipocyte or muscle cell lines
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Calyculin A Plant pathogenic fungi have caused a
2023-08-26
Plant pathogenic fungi have caused a lot of economic losses to agricultural production worldwide every year. It is necessary to develop an bio-sourced antifungal agent for agricultural use. Many researches have shown that the antifungal activity of quaternized chitosan derivatives is mainly affected
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What are the in situ effects of multi site CaM
2023-08-26
What are the in-situ effects of multi-site CaM associations with AT1R? Kai et al. showed that synthetic peptides corresponding to residues 125–137 (rat sequence) in SMD2, 217–227 in the N-terminal side of SMD3, and 304–316 in SMD4JM inhibit to various degrees AngII-induced GTPase activity of isolate
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br AR mediated actions in cells of the
2023-08-26
AR-mediated actions in niclosamide of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discussed els
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br AR mediated actions in cells of the
2023-08-26
AR-mediated actions in LY2874455 of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discussed elsew
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br Experimental Procedures br Acknowledgments br Introductio
2023-08-26
Experimental Procedures Acknowledgments Introduction Cellular and molecular mechanisms underlying synaptic plasticity in the NB-598 are thought to be involved in memory acquisition. Synaptic plasticity is categorised into two main types, long-term depression (LTD) and long-term potentiation
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N terminally extended antigenic peptide precursors that surv
2023-08-26
N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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The metabolism of amino acids into
2023-08-26
The metabolism of amino acids into volatile aldehydes involves both decarboxylation and deamination steps. The order of these reactions and the enzymes performing the catalysis differ among plants [13]. In tomato fruit the conversion of L-Phe to 2-phenylethanal is catalyzed by two enzymatic steps, i
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br Conclusion br Conflict of interest br Acknowledgements
2023-08-26
Conclusion Conflict of interest Acknowledgements Introduction Human salivary aldehyde dehydrogenase (hsALDH) (E.C. 1.2.1.5) is the first line of defence against toxic aldehydes in the oral cavity. HsALDH is primarily a dimeric, class 3 ALDH (ALDH3A1) specific for aromatic and long/medium
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Since the first studies of betaine aldehyde
2023-08-26
Since the first studies of betaine aldehyde oxidation in rats [13], the participation of betaine in the detoxification of homocysteine has well described, considering the activity of other clofibrate as betaine homocysteine methyltransferase and methionine synthase. But, there is a lack of attentio
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Additionally regulation of GPCR heteromerization by specific
2023-08-25
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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