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Hepatic drug metabolizing enzymes and transporters expressio
2021-10-25

Hepatic drug-metabolizing PD 123319 ditrifluoroacetate and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes
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Finally it is possible that the increase in the number
2021-10-25

Finally, it is possible that the increase in the number of EAAT-3-labelled cells in the DG at PD 60, when compared with the control and experimental animals at PD 14, is associated with natural changes in the number of neurons present during the postnatal development of the hippocampus (41, 42) and,
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br The concept of the axo
2021-10-25

The concept of the axo-myelin ‘synapse’ Axons can release glutamate in a Ca+-dependent and independent manner (reviewed in [13,69]). Glutamate released from axons activates GluRs located in myelin, a feature that gave rise to the idea of the axo-myelin ‘synapse’ by analogy with classical synaptic
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A number of anti diabetic drugs are available
2021-10-25

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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GOAT belongs to the super family of membrane
2021-10-25

GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata
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Introduction br Channel activity Since initial
2021-10-25

Introduction Channel activity Since initial reports of the Ca2+-activated K+ permeability of erythrocytes (see Gardos, 1958), several ‘criteria’ have been established to certify K+ fluxes as being due to the Gárdos channel. For example, the requirement for Ca2+ at the intracellular face of the c
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Notwithstanding the functioning of galaninergic system may b
2021-10-25

Notwithstanding, the functioning of galaninergic system may be even more complex (Fuxe et al., 2012). Some studies present evidence that GAL2 receptors might form heteroreceptor complexes with neuropeptide Y1 receptors in 2 deoxy d glucose of amygdala (Narváez et al., 2015a), DRN (Díaz-Cabiale et a
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rifampicin Reports described a range of synthetic GPR agonis
2021-10-23

Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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These agents can be divided into three categories
2021-10-23

These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e
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We have previously established the pharmacokinetic profile a
2021-10-23

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in IMR-1 and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound CID
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Limited efforts were made to exploit the
2021-10-23

Limited efforts were made to exploit the naturally-occurring antigen-specific Treg for ex vivo expansion. This study sets up a reproducible protocol for the expansion of insulin-specific Treg isolated from NOD mice. These XAP044 exhibited higher suppressive capacity compared to the polyclonal Treg
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Diabetes induced damage results in peripheral nerve
2021-10-23

Diabetes-induced damage results in peripheral nerve pathology that BAY 41-8543 correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and peripheral
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It is interesting to note that GlyT and GlyT are
2021-10-23

It is interesting to note that GlyT1 and GlyT2 are modulated in a coordinated and opposite way as that shown in this work by different mechanisms and situations. An example is the purinergic control of GlyT1 and GlyT2 through P2Y receptors in brainstem and spinal cord neurons. This mechanism promote
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Given the proposed importance of
2021-10-23

Given the proposed importance of conformational dynamics to GCK's allosteric regulation, a number of biophysical methods have been utilized to probe the enzyme's dynamic structural landscape. Investigations into the mechanism of 1,3-PBIT dihydrobromide binding, using changes in the enzyme's intrins
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br The actions of GLP on the vasculature
2021-10-23

The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r
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