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In the present study five Glu substituted analogues of GIP
2021-12-03
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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Determination of enzyme activity differs
2021-12-03
Determination of enzyme activity differs from other analytical procedures. In this Guanethidine Sulfate synthesis case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed
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G quadruplex DNA structures may exist
2021-12-03
G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure
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The PK profile and tissue distribution of which has biologic
2021-12-03
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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Introduction Risk factors for colorectal cancer
2021-12-03
Introduction Risk factors for colorectal cancer (CRC) include high-fat diets, sedentary lifestyles, obesity, diabetes, and elevated serum levels of toxic bile acids (BAs) (de Aguiar Vallim et al., 2013, Degirolamo et al., 2011, Downes and Liddle, 2008, Font-Burgada et al., 2016, Kuipers et al., 201
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Hardy et al had demonstrated
2021-12-03
Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited cel
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ampicillin sodium Moreover long term treatment of leukemia c
2021-12-03
Moreover, long term treatment of leukemia cells with imatinib activates AKT, ERK and STAT5 signaling pathway and induce upregulation of EZH2 protein in patients with CML, Ph + ALL and human eosinophilic leukemia cell line (EOL-1 cells) [142]. So, resistance to tyrosine kinase inhibitor (TKI) imatini
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One PKC target that controls cortical actin structure
2021-12-03
One PKC target that controls cortical dhfr inhibitor structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC releases M
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br Experimental br Results br Discussion In this study
2021-12-03
Experimental Results Discussion In this study, we performed molecular docking analysis and in vitro studies to determine whether genistein binds to HIF-1α in BC Okadaic acid and identify the residues involved in this interaction. We found that some functional groups (residues) mimic the bin
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HyperScribe Poly (A) Tailing Kit As indicated by the wide va
2021-12-03
As indicated by the wide variety of pharmaceuticals for IOP management (Table 1), each case of glaucoma is unique and requires a unique treatment regimen to effectively lower IOP. This often results in patients utilizing several medications at once and/or combining medications with surgical interven
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Previously we reported that the inhibition of PKC
2021-12-02
Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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br Materials and methods br Results br Discussion Nervous sy
2021-12-02
Materials and methods Results Discussion Nervous system disease is an important signal of AIDS deterioration (Rosca et al., 2012, Yilmaz et al., 2012). It is possible that HIV crosses the blood in the world barrier or blood cerebrospinal fluid barrier into the central nervous system freely
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br Acknowledgements This work was supported by grants from
2021-12-02
Acknowledgements This work was supported by grants from la Ligue Nationale Française Contre le Cancer « Equipe LNCC 2016 » and Electricité de France RB 2016-17 (to M.S.), NU ORAU (http://www.nu.edu.kz) and Ministry of Education and Science of the Republic of Kazakhstan, program 0115RK03029 (to B.
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Ion dependence of mGluRs activity has
2021-12-02
Ion dependence of mGluRs activity has been previously reported, notably to Ca2+ and Cl− (Kuang and Hampson, 2006). While mGlu1 and mGlu3 receptors were demonstrated to be sensitive to Ca2+, Cl− modulation was reported for all mGluRs, with a lesser extent for the mGlu2 receptor (DiRaddo et al., 2014;
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A general synthesis of the tetrazole is shown
2021-12-02
A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic Epoxomicin followed by reduction of the
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