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As a part of our continuing efforts towards discovery of
2021-12-03
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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For our test subjects we used
2021-12-03
For our test subjects, we used established high fat diet–induced obese (eDIO) male mices T2DM models. The establishment of eDIO mice was accomplished with a 60% high fat diet ad libitum over a 14 week period (initiated at 6 weeks of age). Compared with regularly-dieted mice, the eDIO ones weigh sig
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Manumycin A In skeletal as well as in the heart muscle
2021-12-03
In skeletal as well as in the Manumycin A muscle, the same FBPase isozyme is present (Gizak and Dzugaj, 2003). On the other hand, different isoforms of 6-fructo-2 kinase/fructose-2,6-bisphosphatase (FBPase-2/PFK-2) have been discovered in muscle fibres and cardiomyocytes (Okar et al., 2001, Marsin
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HCV is a highly diverse virus with seven known genotypes
2021-12-03
HCV is a highly diverse virus with seven known genotypes (GT1–7) and multiple subtypes (Gower et al., 2014, Messina et al., 2015, Smith et al., 2014). Patients infected with HCV develop a heterogeneous population of viral species known as quasispecies due to low fidelity of the RNA-dependent RNA pol
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Chronic exposure of cells to cytotoxic
2021-12-03
Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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As preclinical toxicity and efficacy both
2021-12-02
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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Introduction Cancer is known as a
2021-12-02
Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous sglt inhibitors have the ability to bypass the normal apoptosis mechanism (Nati
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br Neural circuits that control
2021-12-02
Neural circuits that control hunger Ghrelin & cognitive control of feeding Ghrelin is a 28 amino marbofloxacin orexigenic peptide that stimulates food intake in rodents and patients (Andrews, 2011, Cummings, 2006, Horvath et al., 2001, Müller et al., 2015, Nakazato et al., 2001, Tschöp et al.
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Amongst oxidants that we have studied PMS is
2021-12-02
Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle Cidofovir [27]. It is interesting to consider why PMS has this effect. PMS funct
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Rink Amide Resin receptor br Presenilins and Wnt catenin sig
2021-12-02
Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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br Declarations of interest br Acknowledgements
2021-12-02
Declarations of interest Acknowledgements This work was supported by the National Natural Science Foundation of China (81673321, 21506099), the State Key Laboratory of Drug Research (SIMM1705KF-13), the Natural Science Foundation of Jiangsu Province (Grant No. BK20151541), and the Jiangsu Syne
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br Materials and methods br Results
2021-12-02
Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta Domiphen Bromide mg [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract,
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Depletion of PI P e g by knockout of PIPKI
2021-12-02
Depletion of PI(4,5)P2, e.g. by knockout of PIPKIγ, also profoundly inhibits SV endocytosis (Di Paolo et al., 2004). Conversely, loss of the PI(4,5)P2-metabolizing PI-phosphatase synaptojanin or its recruitor endophilin stalls SV recycling at the level of clathrin-coated vesicles (Bai et al., 2010,
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A-803467 The most abundant form of Hat p
2021-12-02
The most abundant form of Hat1p in the nucleus is apt to be in the form of the NuB4 complex [96]. In the context of A-803467 assembly, the function of the NuB4 complex may be similar to that ascribed for the cytoplasmic HAT1 complex. That is, the NuB4 complex may be involved in directing newly synth
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Histamine H and H receptor
2021-12-02
Histamine H2 and H3 receptor expression is altered in the CRT0044876 of Hdc mice (Chepkova et al, 2012, Fitzsimons and et al, 2001). Because these mice lack HA, expression of HA receptors might be thought to be irrelevant. This is not the case in Hdc heterozygotes, however, or in patients with a het
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