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A number of anti diabetic drugs are available that inhibit
2022-10-12

A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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Introduction Glucose dependent insulinotropic polypeptide GI
2022-10-12

Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G
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The galactosidase from Aspergillus oryzae is a monomeric
2022-10-11

The β-galactosidase from Aspergillus oryzae is a monomeric enzyme of 113 kDa [58] that has been widely used in GOS synthesis [49,53,[59], [60], [61]], exhibiting a high activity of lactose transgalactosylation [62]. Different immobilization methods have been used for the synthesis of lactose-derived
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As shown in Table the results of
2022-10-11

As shown in Table 3, the results of individual prediction modeling with chemicals at 0.4 mM, 0.6 mM, and 0.8 mM would lead to lesser sensitivity of 60.0%, 65.0%, and 65.0%, respectively, in microsome-unused group, and 85.0%, 85.0%, and 90.0%, in microsome-used group. If we consider only the results
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A majority of aptamer based biosensors termed
2022-10-11

A majority of aptamer-based biosensors (termed aptasensors) is based on structure-switching process of aptamer probes upon target binding [[12], [13], [14], [15]]. And canonical structure-switching aptamer probes are strand-displacement aptamer probes, aptamer beacons and split aptamers [[16], [17],
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br Lung cancer cell lines The greatest expression
2022-10-11

Lung cancer cell lines The greatest expression of both human and rodent FFA4 transcript has been shown to be localized to the lung [61], yet the physiological role in this tissue has been understudied, as has its involvement in lung cancers. In 2015, a two-staged genome-wide association study of
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Natural product based drug discovery can be enhanced with co
2022-10-11

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Q-VD(OMe)-OPh binding assays, we used molecular modeling to predict how well these compoun
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Species specificity of small molecular GPR agonists have bee
2022-10-11

Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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The lack of biological activity
2022-10-11

The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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In addition to FAK P
2022-10-11

In addition to FAK, P-38 MAPK (38 kDa polypeptide) serves as cross-talk effector for signal transduction, enabling this factor to play a vital role in numerous biological processes (Cuenda and Rousseau, 2007). Pharmacologically modulation of P-38 has shown to be an effective approach in the orientat
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Another important question for future studies
2022-10-11

Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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br Results br Discussion Impaired BBB functions evoke
2022-10-10

Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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Evidence demonstrating the interplay between hypoxia and the
2022-10-10

Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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Fig summarizes the results for M concentration of the
2022-10-10

Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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DPP4 Activity Fluorometric Assay Kit synthesis As for hMOF i
2022-10-10

As for hMOF inhibitor's study, Dekker and Zheng et al. synthesized MG149 (Fig. 1) as an inhibitor of Tip60 and MOF which has an IC50 value of 74 ± 20 μM and 47 ± 14 μM [31]. However, MG149 has no experimental data on hMOF in cell or in vivo. The lack of hMOF inhibitor limits the function study of hM
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