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The secretase complex comprises four core subunits presenili
2022-08-02

The γ-secretase complex comprises four core subunits: presenilin (PS), nicastrin (NCT), anterior pharynx-defective 1 (Aph1), and presenilin enhancer 2 (Pen2) [7], [8]. PS is the catalytic subunit of γ-secretase, and many PS mutations associated with familial AD result in a high Aβ42/Aβ40 ratio [5].
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In contrast with the above results in our GC
2022-08-02

In cetp inhibitors with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than mFPR1 in
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Our previous study had shown that silencing
2022-08-02

Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β tipiracil [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti-l
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Accordingly and in animal models
2022-08-02

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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Introduction Histamine H Imidazol yl ethanamine
2022-08-01

Introduction Histamine (2-(1H-Imidazol-4-yl)ethanamine), mol.w. 111.15 g/mol belongs to biogenic amines, which arise in foodstuffs from amino acids by action of microorganism´s or tissue enzymes. Histamine (HA) is formed from the amino VX-745 L-histidine by action of enzyme histidine decarboxylase
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VDAC interacts with hexokinase and is implicated in NLRP act
2022-08-01

VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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The primary physiological role of
2022-07-30

The primary physiological role of the HO system is the protection of beta-Nicotinamide mononucleotide from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degrada
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Atropine In addition to SAHA SBHA also
2022-07-30

In addition to SAHA, SBHA also showed a strong rescue effect. SAHA is a general inhibitor of HDAC function (Finnin et al., 1999, Kim and Bae, 2011), while SBHA is more specific, and has been shown to inhibit HDAC1 and HDAC3 (Richon et al., 1998). The relative level of suppression was similar in Kis
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br Acknowledgments br Introduction Histone deacetylases HDAC
2022-07-30

Acknowledgments Introduction Histone deacetylases (HDACs) related to tumor suppressor genes have become promising targets for the treatment of cancer [1,2]. Under the normal physiological conditions, Histone acetyltransferases (HATs) and histone deacetylases (HDACs) together regulate the acety
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Camptothecin is a type of topo I inhibitor and
2022-07-30

Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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Interestingly interactions between Smad and RhoA the other
2022-07-30

Interestingly, interactions between Smad3 and RhoA, the other small GTPase which is highly homologous to RhoB [9], could not be observed suggesting that the Smad3/RhoB interactions require amino RK-33 residues that are unique to RhoB. Combined with our previous observation that the RhoA gene, which
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AP and NF B activation is inhibited by curcumin
2022-07-30

AP-1 [16], [17] and NF-κB activation is inhibited by curcumin (diferuloylmethane) [18], [19], the yellow component of Curcuma longa that gives curry its colour and flavour. Curcumin has shown anti-inflammatory and antioxidant properties [20], [21], [22], [23], [24], [25], [26] due to the inhibition
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Calcium mobilization FLIPR assay CHO
2022-07-30

Calcium mobilization (FLIPR) assay: CHO-K1 cells expressing an NFAT-β-lactamase reporter and the promiscuous Gα-subunit Gqi5 were stably transfected with either empty vector (pCDNA3.1, Invitrogen) or vector expressing HA-GPR81, GPR109A or GPR109B. Cells were seeded at 10,000cells/well in 384-well cu
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In summary through medicinal chemistry design
2022-07-29

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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br Materials and methods br Results br Discussion
2022-07-29

Materials and methods Results Discussion In the CNS, GLP-1R is associated with G-protein signal transduction pathways, which can activate adenylyl cyclase and protein kinase A by cyclic adenosine monophosphate, and mediates neuronal activities implicated in various pathophysiological change
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