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We next compared the enhancing effects of nM zinc
2021-12-14
We next compared the enhancing effects of 100nM zinc on currents produced by a low concentration of glycine with zinc effects on the same currents produced by the partial agonist taurine. In this experiment, zinc was co-applied with concentrations of glycine or taurine producing 5–10% of the maximal
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While the S site has been
2021-12-14
While the S2 site has been implicated in binding, it SCH772984 is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, there are no c
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Excessive extracellular glutamate can be removed from brain
2021-12-14
Excessive extracellular glutamate can be removed from statins hmg coa reductase inhibitors interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in the blood plas
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Neither GIP nor GIPR SNPs were
2021-12-14
Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib
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br Conflict of interest br Transparency document br Acknowle
2021-12-14
Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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Gadodiamide The objective of this study is to design and syn
2021-12-14
The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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Chemotherapeutic approaches to glioblastoma which
2021-12-13
Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this
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filipin mg Prolonged sGC oxidative inhibition occurs in many
2021-12-13
Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC e
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Activity of compound in rat brain
2021-12-13
Activity of compound 10 in rat TCEP tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as cGMP-depe
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To the best of our knowledge
2021-12-13
To the best of our knowledge, this is the first study to examine functional GSTO1‐1 activity in the cornea. Therefore, comparative data for human or animals is not available. Moreover, we observed the nonspecific degradation of the GSTO1‐1 substrate 4NPG via an unknown mechanism, which was corrected
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Mouse iPSC Chemical Reprogramming Cocktails Kit plus A mutat
2021-12-13
A mutation in stearoyl coenzyme A desaturase 1 gene was reported to reduce sebum production and monounsaturated fatty acids (MUFA) synthesis in mice, which was accompanied with impaired clearance of gram-positive bacteria-induced skin infection (Georgel et al., 2005). Interestingly, gram-positive ba
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In the present studies we found that
2021-12-13
In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 Fluorescein TSA Fluorescence System Kit and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxyg
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Recently they reported an enyne chemotype agonist
2021-12-13
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral g-quadruplex (tmax=15min) and a decent pharmacokinetic profile, a
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As a part of our continuing efforts towards discovery
2021-12-13
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Her
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Mitochondria are also involved in other modalities of progra
2021-12-13
Mitochondria are also involved in other modalities of programmed cell death, particularly apoptosis. Intriguingly, the roles of mitochondria in apoptosis and ferroptosis are fundamentally different. In mitochondria-mediated apoptosis, the mitochondrion serves as a reservoir, storing apoptosis-regula
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