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FFAR is highly expressed not only in
2022-02-11
FFAR1 is highly expressed not only in β cells but also in α angiotensin 2 receptor blocker (Segerstolpe et al., 2016), which gives the interesting perspective that 20-HETE may function both as an autocrine and as a paracrine regulator of islet cell function (Figure 1A), i.e., acting in symphony with
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Multiple mechanisms have been suggested by which glucagon ca
2022-02-11
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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Extensive pharmacological and structural analysis shows GCGR
2022-02-11
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in galeterone 14, 17, 20. Functionally identical to REMD-477, REMD2.59
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In the small intestine digestion and absorption
2022-02-11
In the small intestine, digestion and Capecitabine of the nutrients are the next processes with an impact on the resulting plasma profile. Normally, neither carbohydrate digestion nor absorption are limiting factors, which is illustrated by the rapid and extensive absorption of glucose in condition
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CaCl was from the Radiochemical
2022-02-11
45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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The effect of GC on Fgf was not
2022-02-10
The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 ID-8 was similar in Fgf15+/+ and Fgf15−/− mice. Moreover, GC treatment induced similar Fgf21 up-regulation in both strains. Fxr activation has been reported to increase Fgf21 expression and secretion [28]. In mic
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FXa is a vitamin K dependent serine protease consisting of
2022-02-10
FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 a83 01 synthesis and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. Th
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Together the epigenetic interplay revealed in this study ena
2022-02-10
Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,
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The present experimental study identified remarkable protect
2022-02-10
The present experimental study identified remarkable protective effects for celecoxib against renal toxicity caused by CSA. All aspects of CSA nephrotoxicity, functional, inflammatory, fibrotic, and structural, were improved by celecoxib. Mechanistically, pharmacological and immunostaining protein e
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Computational approaches such as docking and classical
2022-02-10
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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liver x receptor Interestingly the virulence of HBV may adap
2022-02-10
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we pro
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The widespread involvement of HH GLI
2022-02-09
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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In conclusion our work demonstrates for the first time that
2022-02-09
In conclusion, our work demonstrates for the first time that (i) SA-β-gal activity is abundantly present in the gamete cells, such as oocytes and eggs, (ii) the enzyme resides in different cell compartments, (iii) SA-β-gal activity is localized predominantly in acidic endosomal yolk platelets, and (
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The overall very satisfactory potency profile of
2022-02-09
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic daunorubicin australia core in order to improve affinity to FFA1. The agonist activity in this series appears to be par
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Despite the two models for the HIV
2022-02-09
Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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