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Based on the above background gliptins
2020-06-22

Based on the above background, gliptins may exert natriuretic and diuretic effects as well [[112], [119]]. In accordance with this, Girardi and co-workers have demonstrated a physical interplay between DPP-4 and the NHE3 exchanger in the brush-border epithelium of the proximal renal tubule, suggesti
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These data from developing brain are in contrast to noradren
2020-06-22

These data from developing LY364947 are in contrast to noradrenergic receptor regulation in the adult brain. In adult animals, a persistent increase in the α2-AR high affinity state is elicited as a result of DSP-4 lesion or reserpinization, as measured by [3H]clonidine binding to membrane preparat
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Moreover recent structural studies of VEEV nsP pro in comple
2020-06-22

Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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b ng br Early developments Historically the advent of SMEPT
2020-06-22

Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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DDR is one of two
2020-06-22

DDR1 is one of two, non-integrin tyrosine kinase receptors activated by collagen. Although DDR1 has five isoforms (1a, 1b, 1c, 1d, 1e) generated by alternative splicing, only DDR1a and 1b have active kinase domains, whereas DDR2, encoded by a distinct gene, has one isoform (Vogel et al., 2006). Coll
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br Introduction Malaria remains a serious parasitic disease
2020-06-20

Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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Two in vitro reports using lung fibroblasts
2020-06-20

Two in vitro reports using lung fibroblasts have shown that cell transmigration, using transwell migration experiments, through collagen I-coated inserts is mediated by DDR2 and the DDR2-associated signaling kinases JAK2 and ERK1/2, but not DDR1 [63] and that DDR2 regulates the adhesion of fibroblas
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Here we examine the associations between serum
2020-06-20

Here, we examine the associations between serum pro and anti-inflammatory cytokines and cognitive functioning in early-stage bipolar I disorder (BDI) patients. As per previous studies, ‘early-stage’ was defined as being within three years of the first manic episode (Kauer-Sant\'Anna et al., 2009). W
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Compounds and administered orally to fasted Harlan
2020-06-20

Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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br Non cyclic nucleotide EPAC regulators Despite the success
2020-06-19

Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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br Discussion The etiology of autoimmune diseases including
2020-06-19

Discussion The etiology of autoimmune diseases including psoriasis is intricate and a composite of environmental and biological factors. There are very limited studies available that report the association analysis of ACE I/D polymorphism with psoriasis risk. In the current study we report on ass
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Given its high frequency it
2020-06-19

Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant adenosine deaminase to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have b
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NVP-AEE788 Several studies have described the
2020-06-19

Several studies have described the role of NP in vRNP nuclear export. For example, leptomycin B (LMB), an inhibitor of the CRM1 nuclear export signal (NES) binding domain (Kudo et al., 1999), inhibits nuclear export of vRNP and NP, but not NEP or M1, in virally infected or transfected NVP-AEE788 (E
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br Patients and methods br Results Table shows relevant demo
2020-06-19

Patients and methods Results Table 1 shows relevant demographic and clinical characteristics of the 123 patients in the cohort. BAL fluid samples were obtained at a median of 172.5 days after allo-HSCT (range 3 days to five years). Discussion The definitive abandonment of traditional cultu
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To develop antagonists selective for the mouse EP receptor
2020-06-19

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic flavin adenine dinucleotide () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the u
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