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In recent years several DPP IV inhibitors
2022-01-10

In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic BOP reagent with a unique xanthine scaffold developed through high-throug
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While NR upregulation in the
2022-01-10

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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Among the various delivery strategies in the field
2022-01-07

Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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The bFGF induced upregulation of both GR and MR
2022-01-07

The bFGF-induced upregulation of both GR and MR levels observed in our study raises a question regarding whether the simultaneous augmentation of the two receptors has a physiological and/or medical significance. It has been suggested that MR stimulates intracellular signaling pathways to minimize s
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br Ghrelin and energy balance To
2022-01-07

Ghrelin and angiotensin 1 balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identica
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As with the GSIs there are again
2022-01-07

As with the GSIs, there are again major concerns that GSM therapy in patients with symptomatic AD is almost certain to fail, unless the compound has additional mechanism of action not linked to Aβ that prove to beneficial [52]. Although Aβ1–42 or other longer Aβ peptides are critical for initiating
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br Concluding remarks In this small material of thirteen
2022-01-07

Concluding remarks In this small material of thirteen pituitary tumors of various kinds, we could not run statistical analysis. However, with a follow-up period of up to five years, we show that Disclosure Statement Acknowledgments Introduction Galanin is a 29/30-residue neuropeptide fo
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Till date the first line treatment
2022-01-07

Till date, the first line treatment of T2DM is oral metformin followed by oral sulfonylureas, dipeptidyl peptidase-IV-inhibitors, and TZDs. As the disease progresses, injectable glucagon-like peptide-I analogues or ultimately insulin become necessary to maintain glycaemic control. Despite the establ
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The physicochemical properties of the prodrugs provided impo
2022-01-07

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Our observation of LPS induced increase in the
2022-01-07

Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary keap1 nrf2 towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary arteries. However, the possible r
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On the other hand imidazolylcyclopropane derivatives and hav
2022-01-07

On the other hand, imidazolylcyclopropane derivatives and having a 2-substituted benzimidazolyl group showed moderate binding affinities for both the HR and HR. Replacement of 4-chlororbenzylamino group of with a benzimidazolyl group () led to increase the affinity for the HR more than 5-fold ( =
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Several studies have also suggested that Wnt signalling can
2022-01-07

Several studies have also suggested that Wnt signalling can in turn stimulate the transcriptional activity of Yap/Taz (Figure 2, Figure 3). In the Azzolin model, Yap/Taz not only block β-catenin signalling, but their association with Axin1 and/or β-catenin also maintains them in an inactivate state
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br Hedgehog pathway in embryonic development It is
2022-01-07

Hedgehog pathway in embryonic development It is now well established that the Hedgehog pathway solves a role as one of the essential signaling mechanisms for the modulation of cellular growth and differentiation during embryogenesis. Operating through time- and position-dependent mechanisms, this
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Introduction Cancer has been a significant public health pro
2022-01-07

Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve
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thiostrepton Introduction Hepatitis C virus HCV is a small n
2022-01-07

Introduction Hepatitis C virus (HCV) is a small (50–80 nm in size) enveloped RNA virus belonging to the Hepacivirus genus of the Flaviviridae family [1]. The HCV particle consists of a nucleocapsid, which contains the positive single-stranded RNA genome covered by a host cell-derived lipid envelope
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