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br Role of FPRs in regulating the inflammatory response Anne
2021-09-15
Role of FPRs in regulating the inflammatory response Annexin I is a glucocorticoid-regulated protein possessing both pro- and anti-inflammatory activity that might be mediated, in part, by FPR activation [35]. Expressed in a variety of cell types, annexin I is particularly abundant in neutrophils
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Methods Very briefly PLA polymeric nanoparticles as well
2021-09-15
Methods Very briefly: PLA polymeric nanoparticles as well as liposomes were synthesized and loaded with three different FGFR inhibitors. The encapsulation efficiency, average size, PDI, zeta potential, stability and release kinetics were investigated. The most promising formulations were biological
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Type II diabetes is characterized by an inability to maintai
2021-09-15
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty ibotenic acid sale receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors and
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br Materials and methods br
2021-09-15
Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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br Transportation from TGN toward
2021-09-15
Transportation from TGN toward plasma membrane The insulin molecules are packaged along with other molecules such as C-peptides, amylin, Zn2+, ATP and GABA in synaptic-like macrovesicles (SLMVs, with the diameters of 50–100 nm) and large dense core vesicles (LDCVs, with the diameters of 200–500 n
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In vitro studies have described
2021-09-15
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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br Discussion This study dedicated to histamine H and H
2021-09-15
Discussion This study, dedicated to NG25 H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transmitter rel
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Multi targeting agents are of major
2021-09-15
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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br Hippo pathway signalling The Hippo pathway is an
2021-09-15
Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular hippo signaling status [10]. This pathway is linked to development, cell prol
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Interestingly the virulence of HBV may
2021-09-15
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we pro
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br Conclusions br Acknowledgments This work
2021-09-15
Conclusions Acknowledgments This work was financially supported partly by Shanghai Pujiang Talent Project (No.: 08PJ14017), the National Natural Science Foundation of China (Nos.: 20771029 and 91013001) and Shanghai Leading Academic Discipline Project (No. B108). Soluble guanylate cyclase (
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br Material and methods br Results and discussion Unlike
2021-09-15
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 STF 083010 synthesis biosynthesis and an increase in respiration, pepper fruits, which do not follow this pattern, are called n
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Bupivacaine is one of the local anesthetics commonly
2021-09-15
Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root Pam3CSK4 (DRG) neurons [5], [6], [7],
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The stress of accelerated lactate production in cancer
2021-09-15
The stress of accelerated lactate production in cancer adenosine monophosphate is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport depending on the environment
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In summary through medicinal chemistry design and computer a
2021-09-14
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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