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One possible pitfall of using EPAC activators in
2021-04-20

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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br Conflicts of interest br Financial
2021-04-20

Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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Propylthiouracil In conclusion we propose that UBE T FANCT m
2021-04-20

In conclusion, we propose that UBE2T (FANCT) mutations define a FA subtype. This is also a rare example of a mutated E2 enzyme causing an inherited human disorder, like UBE2A. The p.Gln2Glu substitution is probably hypomorphic, as indicated by the fact that a siUBE2T knockdown made AP65P-hTERT Propy
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In this paper we describe a facile and
2021-04-20

In this paper, we describe a facile and universal method for in situ crosslinking of DNA micelles, using spherically directed reduction of metal ions. As shown in Scheme 1A, a single-stranded DNA (ssDNA) consisting of a ligand domain, a template domain, and a lipid domain was designed as a monomer t
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SCH-900776 synthesis Three DDR binding sites have been mappe
2021-04-20

Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG
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Two in vitro reports using lung fibroblasts have
2021-04-20

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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Henderson et al reported that allergen
2021-04-20

Henderson et al. [20] reported that allergen-induced airway remodeling was blocked by the CysLT1 receptor antagonist montelukast. The development of epithelial thickening and mucus accumulation at relatively small bronchi was also suppressed by montelukast. The CysLT2 receptor antagonist BayCysLT2RA
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Ethyl naphthoates a h were successfully reduced
2021-04-20

Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The
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Epalrestat br Advantages of modified proteins
2021-04-19

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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BH3I-1 synthesis Organ fibrosis is thought to be initiated b
2021-04-19

Organ fibrosis is thought to be initiated by repeated or chronic epithelial injury. The current belief is that damaged epithelial BH3I-1 synthesis induce an aberrant and unresolved wound repair process by activating fibroblasts via various profibrotic cues. Upon injury, epithelial cells activate th
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br Concluding remarks Some of the
2021-04-19

Concluding remarks Some of the clinical trials of putative neutral competitive ERAs have been less successful than anticipated 6, 8, 11. This might be because of underestimation of the complexity of the molecular pharmacology of ETA. To resolve this, it will be necessary to define the signaling m
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br Results br Discussion Fetal development occurs under cond
2021-04-19

Results Discussion Fetal development occurs under conditions of low oxygen tension and steady maternal glucose such that physiologic systems including the pancreas are functionally poised in the prenatal state. Postnatally, oxidative metabolism becomes dominant and intermittent feeding exposes
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Pioglitazone HCl The Liver X Receptor and LXRs NR
2021-04-19

The Liver X Receptor-α and -β (LXRs, NR1H3 and NR1H2, respectively) are members of the nuclear receptor superfamily that play a central role in controlling cholesterol homeostasis [9], [10]. In macrophages, LXRs can decrease the cellular sterol burden by inducing expression of the cholesterol efflux
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Our research has demonstrated that the absolute bioavailabil
2021-04-19

Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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br EBV Infection Epstein Barr virus
2021-04-19

EBV Infection Epstein–Barr virus (EBV, human herpesvirus 4) was discovered 50 years ago, when Epstein, Achong, and Barr used electron microscopy to identify viral particles in Burkitt's lymphoma cells. It belongs to the lymphocryptovirus (LCV) genus of the gammaherpesvirus subfamily (Fig. 1A). Th
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