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GK allosteric activators validate the importance of GK from
2022-02-18
GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many
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br Materials and methods br Results
2022-02-18
Materials and methods Results Discussion Common to catfish fry production, high stocking densities as well as intensive handling during transport can result in low dissolved oxygen levels (Abdalla and Romaire, 1996; Torrans et al., 2003), which can result in fish stress. It is not known at
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In a mouse model of hyperhomocysteinemia a risk factor
2022-02-18
In a mouse model of hyperhomocysteinemia (a risk factor for the development of vascular dysfunction) it has been shown that myoendothelial communication is enhanced due to increased expression of Cx37 and IK1 624 [], allowing the propagation of endothelial signals to VSMC and thereby decreasing the
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Introduction Osteoclasts are large multinuclear cells that a
2022-02-18
Introduction Osteoclasts are large, multinuclear rad51 inhibitor that are responsible for the resorption (breakdown) of bone [1]. Together with osteoblasts, the bone forming cell, they maintain the integrity of the skeleton through constant resorption and repair of bone. Osteoclast precursors of m
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br Conflicts of interest br Acknowledgment br Introduction
2022-02-18
Conflicts of interest Acknowledgment Introduction The Ro 48-8071 growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years [1], [2]. This family
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br G protein coupled receptor GPR also known as a
2022-02-18
G-protein coupled receptor 40 (GPR40), also known as a free fatty mecamylamine synthesis receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that GPR4
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At the heart of ferroptosis
2022-02-18
At the heart of ferroptosis is a process of lethal lipid peroxidation, which is the oxidative addition of molecular oxygen (O2) to lipids, such as polyunsaturated fatty acyl tails in phospholipids. The first descriptions of such enzymatic reactions were in 1955 by Peterson and colleagues [50] and Ro
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Following these discoveries the term ferroptosis was coined
2022-02-18
Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de
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Introduction of a chloropyridine group
2022-02-18
Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels
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br Conclusions and perspectives br Acknowledgements This
2022-02-18
Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025
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The synthesis of substituted pyrimidinone
2022-02-18
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of hpdp provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford inseparable m
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Computational approaches such as docking and classical molec
2022-02-18
Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over
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It has been demonstrated that
2022-02-18
It has been demonstrated that RA regulates gene 5 03 through an epigenetic mechanism during stem cell and cancer cell differentiation. In neuroblastoma cells, RA induced neural maturation through RET gene transcriptional activation by increasing H3K4me3 levels at the promoter region and demethylatin
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In T cells whereas SETDB is implicated
2022-02-18
In T cells, whereas SETDB1 is implicated in OX40-dependent repression of the Il17a locus in Th17 cells (Xiao et al., 2016), SUV39H1 controls Th2 cell stability by depositing H3K9me3 at the Ifng promoter (Allan et al., 2012). However, the deregulation of the Ifng locus observed in Suv39h1−/− cells ca
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Based on the inhibitory potency of C for HDAC we
2022-02-18
Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o
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