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telomerase inhibitors Recently unimolecular multi functional
2021-12-08
Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with telomerase inhibitors and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control
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Moreover the ubiquitous expression of the OTR and
2021-12-08
Moreover, the ubiquitous leukotriene of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased signalling asso
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Murine models of sickle disease have been
2021-12-08
Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot
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Amongst oxidants that we have
2021-12-08
Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle PDK1 inhibitor [27]. It is interesting to consider why PMS has this effect. PMS
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In addition to the type of
2021-12-08
In addition to the type of food consumed, also the effect of calorie restriction (CR), i.e. an intermittent fasting and re-feeding cycles with concomitant fluctuations in the level of glucose and insulin, can affect the course of IBS through the modulation of the BA homeostasis. This type of nutriti
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The pharmacokinetic properties of were
2021-12-08
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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Sumoylation of transcription factors has been generally
2021-12-08
Sumoylation of transcription factors has been generally linked to transcriptional repression and, in a few cases, to transcriptional activation [60] Accumulating evidence implies that corepressor complex subunits, including CoREST, CtBP, Daxx, NCoR1, SMRT and histone deacetylase complexes (HDACs), p
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The synthesis route of strobol C started from kirenol which
2021-12-08
The synthesis route of strobol C started from kirenol, which was treated with phosphomolybdic 2-Deoxyadenosine 5-diphosphate hydrate in acetone to afford isopropylidenkirenol () as illustrated in . Treatment of with acetic anhydride in a mixture of dry pyridine, gave fully protected intermediate
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br Recently MST emerged as a critical regulator
2021-12-07
Recently, MST1 emerged as a critical regulator of leukocyte function and autoimmunity in humans. Five independent groups reported on autosomal recessive nonsense mutations in the gene STK4 (which encodes for MST1) in human patients with a novel primary immunodeficiency disease (PID), now called ST
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Recently IL was also identified as
2021-12-07
Recently, IL-10 was also identified as an important mediator of collagen deposition in the development of HF [64,65]. It was shown, that this cytokine activates macrophages found in the hearts of mice suffering from diastolic dysfunction in the autocrine manner [64]. In response, specific subset of
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A two way chi square test was
2021-12-07
A two-way chi-square test was used to determine statistically significant differences between corresponding frequencies of GT results for the 2 testing periods. A p value of Results Distribution of HCV GT results obtained during the 2 study periods are shown in Table 1. While very low frequencies
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Our last area of exploration was the piperidine core as
2021-12-07
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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lipoxygenase inhibitor The precise mechanisms of action of
2021-12-07
The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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br Investigations br Genetics GLUT is a
2021-12-07
Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, NVP-BEP800 microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, located on chrom
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GLI proteins activate or repress transcription of their
2021-12-07
GLI proteins activate or repress transcription of their target genes by binding to a similar sequence motif within a cis-regulatory module (CRM) (Hallikas and Taipale, 2006, Peterson et al., 2012). Transcriptional responses to the HH pathway can be elicited either by de-repression of GLI-R or in oth
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