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The LNX ligand of numb protein X or
2020-04-26
The LNX (ligand of numb protein-X) or PDZRN (PDZ and RING) family of proteins consists of five members (LNX1–LNX5), the first four of which act as E3‐ubiquitin ligases in various roles, as reviewed elsewhere [14]. LNX proteins comprise a RING domain and two to four PDZ (PSD-95, DlgA, ZO-1) domains [
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We have compared the potency of a
2020-04-26
We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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br Discussion Of the age related differences in
2020-04-26
Discussion Of the age-related differences in serum non-cholesterol sterols, we first deal with the cholesterol precursors. After birth, the markedly elevated serum desmosterol values decreased during the first year of life, and after 1 year of age they were similar between the other age groups. S
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br O GlcNAcase Human OGA is
2020-04-26
O-GlcNAcase Human OGA is a multidomain protein with an N-terminal domain similar to glycoside hydrolase family 84 (GH84) enzymes, a stalk domain, a C-terminal pseudo histone acetyltransferase (HAT) domain, and several low-complexity regions (Figure 1f) [43]. A splice variant that lacks the HAT do
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Damage of PE HD due
2020-04-26
Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o
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Mouse Cyp a is a
2020-04-26
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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Methimazole The imbalance that renders greater lipid
2020-04-26
The imbalance that renders greater lipid uptake toxic is unclear, but the comparison of our in vitro studies with those in mice illustrates the importance of TAG storage versus accumulation of less non-polar molecules. Protective effects of ACSL1 and PPARγ have been reported in other cell types. Par
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ICT is a product of icariin via the
2020-04-26
ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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br Discussion Several DPP inhibitors are currently available
2020-04-26
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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Herein the interactions of etamicastat nepicastat and zamica
2020-04-26
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the rapamycin buy exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP re
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br Acknowledgements We thank Dr Tai Yuan Yu
2020-04-26
Acknowledgements We thank Dr. Tai-Yuan Yu and Miss Chun-Ping Chang for helping with the drug/DNA sequence specificity study. We also thank the Chemical Synthesis Core and the Pathology Core Laboratory of IBMS for synthesizing SL-1 and for performing the pathology analysis, respectively, and the T
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A spectrum of therapies came
2020-04-26
A spectrum of therapies came in order to counter this misfortune, some of them are discussed below. However, the common problem faced by most of these drugs is their emerging resistance after a span of time. Some of the important drugs reported so far are as: Quinine-based antimalarial drugs (Fig. 1
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Present malarial chemotherapies mainly rely on a very few ch
2020-04-26
Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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Posaconazole Published results have revealed relationships b
2020-04-24
Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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Though limited to a large cohort of self reported
2020-04-24
Though limited to a large cohort of self-reported healthy individuals, associations between individual Mefloquine hydrochloride have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predic
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