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Compared to methadone or morphine buprenorphine is
2022-07-19
Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve
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Through a large scale phylogenetic
2022-07-19
Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 10Panx can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubacteria g
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br Materials and methods br Results
2022-07-19
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the egfr inhibitors of neurons and
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MRcKO mice showed a comparable degree of cardiac
2022-07-19
MRcKO mice showed a comparable degree of cardiac remodeling compared to control (MRf/f) mice. Moreover, the worse cardiac remodeling in pressure-overloaded GRcKO mice is not due to compensatory activation of cardiomyocyte MR, because GRMRdcKO mice displayed cardiac remodeling to the same extent as G
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Here we examined whether complete
2022-07-19
Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Somatostatin analogues are among the
2022-07-19
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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This hypothesis is in line
2022-07-18
This hypothesis is in line with our phylogenetic analysis of FBPase sequences which revealed that vertebrate FBP2 evolved significantly faster than FBP1 (Fig. 2). An average distance between FBP2 and ancestral vertebrate FBPase was higher than that for FBP1. Moreover, preliminary study on amphibia
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br Acknowledgments This research was supported by the
2022-07-18
Acknowledgments This research was supported by the National Institutes of Health Grants GM58442 and GM084152, as well as the National Institutes of Health Predoctoral Training Grant 5T32GM008700-13. We thank Eric Oldfield (University of Illinois, Urbana-Champaign) for providing the FDPS inhibitor
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Conformational analysis provides further insight into the
2022-07-18
Conformational analysis provides further insight into the SAR trends apparent in . Acyclic precursors – are 25–50-fold less active than their macrocyclic counterparts – against Pyk2. The global minima for – are conformations in which the –NHCH– linker between the pyrimidine and pyridine rings is sta
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FXa is a vitamin K dependent serine protease consisting of
2022-07-18
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 monocarboxylate transporters and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel struc
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br Acknowledgment br Introduction Non steroidal anti inflamm
2022-07-18
Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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Several mechanisms have been suggested to underline the
2022-07-18
Several mechanisms have been suggested to underline the release of signalling molecules from astrocytes: reverse operation of glutamate transporters, volume-regulated anion channels, gap-junctional hemi channels, diffusional release through purinergic receptors and Ca2+-dependent exocytosis [2], [15
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The dramatically reduced expression of CFTR in human
2022-07-18
The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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We found that activator drugs
2022-07-18
We found that activator drugs decrease NOsGC protein levels in Sf9 cells. This decrease in protein levels is more pronounced for BAY 60–2770 compared to cinaciguat, and more obvious for α1/β1 compared to α2/β1 (see Fig. 2). This led us to hypothesize that the reduction in protein level correlates wi
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As a result of the capability of modulating
2022-07-18
As a result of the capability of modulating the dynamic changes and rearrangement of cytoskeletons, the Rho GTPases, in which RhoA, Cdc42 and Rac1 are best-characterized, have been highlighted as significant contributors for orchestrating neuronal development (Duman et al., 2015, Heasman and Ridley,
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