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We have previously established the pharmacokinetic profile a
2021-09-02
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in TDZD-8 and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound CI
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In addition researchers studying GPR
2021-09-02
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it Amsacrine is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (
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br Materials and methods br Results br Discussion
2021-09-02
Materials and methods Results Discussion The GO system is an important mechanism for maintaining the integrity of genetic material in many eukaryotic organisms. This is demonstrated by the high conservation, across different evolutionary lineages, of the sequences of the proteins that compo
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Excessive extracellular glutamate can be removed from brain
2021-09-02
Excessive extracellular glutamate can be removed from NVP-ADW742 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 plasma increases in case of is
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Free d glutamate also has been found
2021-09-02
Free d-glutamate also has been found in various tissues of invertebrates and vertebrates including mammals (Han et al., 2011; Ariyoshi et al., 2017), fish (Kera et al., 2001) amphibians (Kera et al., 2001), birds (Kera et al., 2001), mollusks (Tarui et al., 2003; Patel et al., 2017) and arthropods
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Peripheral injury or disease induced alterations
2021-09-02
Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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br Factor Xa an enzyme in the coagulation
2021-09-02
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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br E intracellular localization br Regulation
2021-09-02
E1 intracellular localization Regulation of E1 by other post-translational modifications Concluding remarks Acknowledgments We apologize to those whose work was not included because of space considerations or whose papers were unintentionally omitted. We thank Dr Peter Bullock (Tufts Uni
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Treatment related adverse events have been
2021-09-01
Treatment-related adverse events have been a serious issue in clinical application. Severe toxicity has been reported in clinical trials using antibody blockade of CSF-1R (20 mg/kg), PD-1, and CTLA-4.29, 30, 31 However, apparent side effects were not observed in our study with PLX3397 treatment alon
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br Author contributions br Conflicts of interest br Introduc
2021-09-01
Author contributions Conflicts of interest Introduction Current the 5-year survival rates for lung and pancreatic cancers are 18% and 8%, respectively. These low survival rates are partially because of the late diagnosis of one-half of cases, in which 5-year survival decrease to 4% and 3%,
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br Acknowledgments br Introduction Cell cycle arrest
2021-09-01
Acknowledgments Introduction Cell cycle arrest or delay may occur at 3 major checkpoints, i.e. G1/S, intra-S and G2/M. p53 has a central role in controlling the G1/S checkpoint, and its loss or deactivation, occurring in the majority of cancers, forces cancer cells to rely on the S and G2/M ch
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Raloxifene is a second generation SERM that has tissue speci
2021-09-01
Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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Lavallee et al reported that PREG
2021-09-01
Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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For most enolases fluoride acts as an inhibitor while Mg
2021-09-01
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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Upon assembly of HLA tetramers loaded
2021-09-01
Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T acetylcholine chloride recognizing the respective peptide-HLA complexes. We found no significant difference in fr
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