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The highest metabolic stability observed
2022-04-25
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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The ultimate success of multimodal probe in the inflammation
2022-04-25
The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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Under normal physiological conditions the body has sufficien
2022-04-22
Under normal physiological conditions, the body has sufficient oxygen supply, so glucose can produce large amounts of ATP by aerobic oxidation and oxidative phosphorylation in cells. After SCI, hypoxia ischemia can occur in local tissue, leading to decreasing of intracellular oxygen partial pressure
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In the previous study concerning HO mediated inhibtion of
2022-04-22
In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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Z-WEHD-FMK br Structural studies of GCAP Recoverin was the f
2022-04-22
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding Z-WEHD-FMK to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The cryst
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The Scribble complex localizes to the leading edge in
2022-04-22
The Scribble complex localizes to the leading edge in response to integrin engagement. There, Scribble controls the activation Rac and PAK via the Rac GEF β-Pix (Bahri et al., 2010), which is required for collective cell migration (Omelchenko et al., 2014). However, on the rear edge, Scribble can be
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Acknowledgments br INTRODUCTION AND OBJECTIVES br METHODS br
2022-04-22
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. B
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Recent evidence suggests that HCA can also mediate antineuro
2022-04-22
Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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br Acknowledgments We thank Dr Kathleen Sullivan of Merck
2022-04-22
Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 DRB expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andrew Howard
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The diseases of ocular surface
2022-04-22
The diseases of ocular surface and the cornea are very common in ophthalmological practice and as a result there is a continuous, need for novel therapeutic options. Here, we demonstrated a corneal distribution of GPR35, a potential molecular target for new drugs (; ). The search for the expression
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In our study we evaluated adenovirus type Ad
2022-04-22
In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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In the present study both experimental and theoretical studi
2022-04-22
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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Always some extra effort may make great progress
2022-04-22
Always, some extra effort may make great progress in sensing platform, for example, Ma's group discovered luminescent iridium (Ⅲ) complexes which were highly selective for G-quadruplex DNA and Al3+, then they utilized these complexes to develop a series of G-quadruplex-based probes and chemosensor r
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br Glycoprotein Production br Strategies to Obtain Glycoprot
2022-04-22
Glycoprotein Production Strategies to Obtain Glycoprotein Compositional Homogeneity Glycoproteins are modified by glycosyltransferases and glycosylhydrolases in the ER and Golgi; however, the degree of remodeling for each glycan on each protein is not explicitly defined by a template (Moremen
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Post translational ubiquitination has been shown
2022-04-22
Post-translational ubiquitination has been shown to regulate a wide range of cellular responses, such as the synaptic trafficking and turnover of neurotransmitter receptors (Rape, 2018). Ubiquitination is also engaged in the modification of protein-protein interaction and intracellular signaling tra
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