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MDL 28170 Recently competitive inhibitors of arginase have
2025-01-23

Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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TSA assay br The pathogenesis of AD and the targets of apeli
2025-01-23

The pathogenesis of AD and the targets of apelin Alzheimer's drugs Conclusions Introduction APJ, first identified from a human genomic library in 1993, belongs to a member of seven trans-membrane G protein-coupled receptor family. Its amino TSA assay sequence has 31% homology with that o
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Apelin is involved in various
2025-01-23

Apelin is involved in various physiological functions, including Losmapimod contraction (Ashley et al., 2005), vasodilatation (Jia et al., 2007), feeding control (Valle et al., 2008), and metabolic homeostasis (Higuchi et al., 2007, Dray et al., 2008, Attane et al., 2010). Its plasma level is eleva
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Phenolic compounds show reciprocal relationship with colonic
2025-01-23

Phenolic compounds show reciprocal relationship with colonic microflora. Phenolic compounds are able to improve colonic health and modulate microbiota diversity with prebiotic and antimicrobial functions, while colonic bacterial enzymes catalyze deconjugation, dehydroxylation, and convert phenolic c
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Therefore we have further investigated the
2025-01-23

Therefore, we have further investigated the anti-oxidant activity of isogarcinol in vitro by measuring the scavenging of 2,2′-diphenyl-1-1picrylhydrazyl (DPPH) and 2,2′-azino-bia (3-ethylben-zothiazoline-6-sulphonicacid) (ABTS), and determining its reducing power and ability to prevent lipid peroxid
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Of the cardiovascular studies involving
2025-01-23

Of the cardiovascular studies involving ARBs, 3 reported renal outcomes. In the Losartan Intervention For Endpoint study, albuminuria was observed less frequently in the losartan than in the atenolol arm (7% vs. 13%; p=0.002) (5). In the Candesartan Antihypertensive Survival Evaluation in Japan tria
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In order to postulate its binding mode in APN
2025-01-23

In order to postulate its binding mode in APN, GDC-0084 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by the
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Kuda et al reported that the activity
2025-01-23

Kuda et al. (1997) reported that the activity of aminopeptidase A (ApA) but not aminopeptidase B (ApB) nor aminopeptidase N (ApN) was decreased in plasma from patients with Alzheimer's disease (AD). More recently Puertas et al. (2013) reported that the activities of plasma ApA, ApB, ApN and IRAP wer
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Based on our findings in this work as well as
2025-01-23

Based on our findings in this work as well as the previous published data in the experimental mice model of RSV infection, we suggest that modulation of 12/15 LOX expression and/or blocking of LOX products such as 12(S)-HETE may represent potential pharmacological approaches to prevent or treat vira
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Various compounds have been designed to inhibit aldose
2025-01-23

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic PF-3758309 moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a pot
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PSI-7977 mg Flavonoids protein interactions studies play a s
2025-01-23

Flavonoids-protein interactions studies play a substantial part in the hunt for novel molecules which are to interact with a selected disease-relevant target [35]. The mode of potential interaction gives information about the flavonoid effectiveness and selectivity. Lately, possible target molecules
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proanthocyanidin The putative physiological meaning of epine
2025-01-22

The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c
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br Discussion With recently improved understanding of the ro
2025-01-22

Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e
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NSC 652287 In this article we have outlined
2025-01-22

In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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The results also showed that the A receptor http www
2025-01-22

The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 NF-κB activation blocker stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transe
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