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The usefulness of GIP R antagonism for
2021-10-15
The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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Recently the classical view of the compartmentalization
2021-10-14
Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic Thiomyristoyl (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, the las
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MMV s distinct mode of inhibition addresses key impediments
2021-10-14
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Here we show that Hippo signaling components are expressed d
2021-10-14
Here, we show that Hippo signaling components are expressed during epicardium formation. To determine the significance of Yap and Taz in the developing epicardium, we generated epicardium-specific Yap/Taz double-knockout mice. Genetic deletion of Yap and Taz using Sema3d mice leads to embryonic leth
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br Introduction Although effective hepatitis B virus
2021-10-14
Introduction Although effective hepatitis B virus (HBV) vaccines are in use worldwide, HBV-related liver diseases are still a major public health concern, causing considerable morbidity and mortality. Approximately 257 million people are currently suffering from chronic hepatitis B and 887,000 de
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2021-10-14
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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br Materials and methods br Results As
2021-10-14
Materials and methods Results As expected, due to matching by age, the mean ages were similar for the two groups of children when stratified by ASD status; children with an ASD had a mean age of 67.0 months, while the mean age for children in the TD control group was 68.0 months. Nearly all of
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Glutathione in reduced form GSH the tripeptide glutamyl cyst
2021-10-14
Glutathione in reduced form (GSH, the tripeptide, γ-glutamyl cysteinyl glycine) is a non-enzymatic low-molecular-weight antioxidant necessary for the maintenance of a cellular redox state (Noctor et al., 2012). At the stage of the transition from germination to seedling growth the process of cell di
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br Medium and long chain fatty
2021-10-14
Medium- and long-chain fatty cam kinase ii receptors Clinical studies of ω3 fatty acids Clinical studies have established that dietary intake of ω3 fatty acids should be around 4g/day for treating very high triglyceride levels (≥5.7mmol/L) [36]. Low-dose supplementation with EPA + DHA (400mg/
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Apart from the different assays used
2021-10-14
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 wnt inhibitor stably transfected with human GPR55. They found that the effect of both ligands on intracellular Ca2+
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br Acknowledgments This work was supported by
2021-10-14
Acknowledgments This work was supported by the National Institutes of Health (R01 A1084898) to M.V. Williams and M.E. Ariza. Introduction Female pattern hair loss (FPHL) has emerged as the preferred term for androgenetic alopecia (AGA) in women due to the uncertain relationship between andro
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In conclusion we have designed
2021-10-14
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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In the present study we set out
2021-10-14
In the present study we set out to discover new non-steroidal SEGRA and to analyse their mechanism of function. Towards this goal we initiated a virtual screening (VS) approach, utilizing structure-based pharmacophore modeling, in silico docking and molecular dynamics (MD) simulations. Our pharmacop
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Introduction Parkinson s Disease PD is a neurodegenerative
2021-10-14
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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Using data from a large population
2021-10-14
Using data from a large population-based cohort study in Finnish males and females, Suchankova et al. [97] looked at a subset of the aforementioned SNPs, namely one SNP on GHSR (rs2948694) and two SNPs on GHRL (rs4684677 and rs696217), in relation to alcohol use disorders identification test (AUDIT)
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