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The suboptimal trypsin selectivity profile of DPC p
2022-07-15
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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br Anandamide signaling and cardiovascular function The card
2022-07-15
Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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To date the crystal structures
2022-07-15
To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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Dehydroepiandrosterone receptor While reduced protein synthe
2022-07-15
While reduced protein synthesis provides a model to explain the long-term memory defects of kdm5 and kdm5 flies, new translation is not required for short-term memories. The chronic reduction in translation observed in mutant fly strains may, however, lower the levels of proteins necessary for short
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p neurotrophin receptor p NTR or CD a
2022-07-15
p75 neurotrophin receptor (p75NTR or CD271), a member of the tumor necrosis factor receptor superfamily, has been implicated in several steps of glioma tumorgenesis [5]. p75NTR mediates glioma invasion and progression through γ-secretase-dependent and -independent mechanisms [6], [7], and its expres
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fgf receptor inhibitor Thus regardless of its specific funct
2022-07-15
Thus, regardless of its specific function, PTC52 is associated with plastid activity. During arbuscular mycorrhizal symbiosis, elongated plastids, which are interconnected through thin, tubular plastid projections called stromules, proliferate in arbuscule-containing root cortex cells (Fester et al.
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Small but statistically significant variance in PhyChem inde
2022-07-15
Small but statistically significant variance in 7 PhyChem indexes measured using intra-host HVR1 variants was shown to be strongly associated with CIP and MIP. All HVR1 sequences (N = 28,622) used here share only 6782 profiles of the selected 29 DAC’ of 7 PhyChem indexes. The significant majority (
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br Other mechanisms In vitamin B
2022-07-15
Other mechanisms In vitamin B6 deficiency, antibody production may be indirectly impaired [38]. Grindley et al. [4] showed that high dietary intake of vitamin B6 (74.3 mg PN/kg diet) suppresses herpes simplex virus type 2 transformed cell-induced tumor growth and enhances immune status compared w
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Multiple studies from our laboratory
2022-07-15
Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various
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br Material and methods br
2022-07-15
Material and methods Results and discussion Unlike many fruits such as bananas and tomatoes, known as climacteric fruits, in which ripening is regulated by a burst of Reversine biosynthesis and an increase in respiration, pepper fruits, which do not follow this pattern, are called non-climact
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Acknowledgments br INTRODUCTION AND OBJECTIVES br METHODS br
2022-07-15
Acknowledgments INTRODUCTION AND OBJECTIVES METHODS RESULTS CONCLUSIONS Introduction Class 3 alcohol dehydrogenase (EC 1.1.1.1), also known as ADH5 chi polypeptide in humans, was first identified by Koivusalo et al. [1] as a NAD+-dependent hydroxymethylglutathione (HMGSH) oxidase. By
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In the pathogenesis of insulin
2022-07-15
In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph
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A few of the islet
2022-07-15
A few of the islet-specific proteins identified in the present study have previously been described in various contexts of pancreatic islets, i.e. PTPRN, SCG5, SCGN, SNAP25 and SNED1, validating the search algorithm applied and supporting the notion that also the novel proteins identified are indeed
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(R)-(+)-Etomoxir sodium salt synthesis The GPR receptor is a
2022-07-15
The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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In summary through medicinal chemistry design and
2022-07-15
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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