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Lastly haspin inhibitor was assessed against a panel of
2022-08-03

Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the bay 11 inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DYRK1B, DYRK3, PASK, PIM1 and PKD3. Inter
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br Conclusion br Acknowledgements This work
2022-08-02

Conclusion Acknowledgements This work was supported by a Grant-in-Aid for challenging Exploratory Research (15K12715) and was a partly supported by Suzuken Memorial Foundation (2014). The authors would like to thank Enago (www.enago.jp) for the English language review. G protein-coupled rec
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Cichlasoma dimerus as most teleost fish species present
2022-08-02

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most Amphotericin B synthesis species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and th
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Tanshinone IIA---sulfonic sodium mg Entry into CNS is tightl
2022-08-02

Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of th
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To confirm that these were bona fide interactions
2022-08-02

To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5
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His brother individual B II is months old He was
2022-08-02

His brother, individual B.II-4, is 11 months old. He was born at term with intrauterine growth retardation. His birth weight was 2.2 kg (T (p. Arg176Trp) variant in SLC45A1 (GenBank: NM_001080397.1). This variant is very rare (MAF = 0.00001660 in the ExAC Browser) and predicted to be damaging by Pol
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A key limiting factor in
2022-08-02

A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of Phos-tag of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessit
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In the present study five
2022-08-02

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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The molecular nature of these putative Ca channels is at
2022-08-02

The molecular nature of these putative Ca2+ Protease Inhibitor Library is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which were characterized as B-channels, se
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br Conclusions There are a number of factors that affect
2022-08-02

Conclusions There are a number of factors that affect the transit of solutes through gap junction channels. Fig. 4 provides a simplified illustration of those factors. First is the cytoplasmic vestibule through which all permeable solutes must pass to gain access to the pore. In an equivalent cir
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Knock out mice of FXR showed enhancing cholesterol metabolis
2022-08-02

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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endothelin receptor antagonist The PK profile and tissue
2022-08-02

The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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The highest metabolic stability observed for compound k
2022-08-02

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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FFAs concentration response curves for increasing intracellu
2022-08-02

FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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dihydrofolate reductase inhibitor GLP is released in respons
2022-08-02

GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty dihydrofolate reductase inhibitor receptor 4 (FFA4/GPR120) as a potential 7
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