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Rifampicin that is methyl piperazinyl imino methyl rifamycin
2022-04-06
Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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Two intermediate compounds A and B in Fig
2022-04-06
Two intermediate compounds (A and B in Fig. 1) were tested for both Aβ40 and CYP3A4 inhibition activity. Potential hydrolysis of structures I and IIin vivo may produce A which is a strong CYP3A4 inhibitor. Cyclopropanol group is a suspected liability, because Hexa His B without it has a clean CYP3A
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The focused set of additional pyrazole analogs
2022-04-06
The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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A way to identify what subunit interfaces contribute to
2022-04-06
A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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The effect of on the conformational of G quadruplexes was
2022-04-06
The effect of on the conformational of G-quadruplexes was investigated with circular dichroism (CD) spectroscopy. In the absence of , the CD spectra of parallel G-quadruplex exhibited a characteristic positive peak at about 265 nm, and a negative peak at about 240 nm; antiparallel G-quadruplex sh
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br Results br Discussion Glucose
2022-04-06
Results Discussion Glucose homeostasis is regulated by a complex and intricate signaling network involving multiple organs. The BA nuclear receptor FXR is integrated into this regulatory network and participates in glucose handling and metabolism. Intestinal FXR favors glucose CID 755673 and
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FPR ligands comprise structurally very diverse classes
2022-04-06
FPR ligands comprise structurally very diverse ARQ197 of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolones, pyridazine-3
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Not only has the cortical actin network
2022-04-02
Not only has the cortical 2 types of active transport network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositi
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In T cells whereas SETDB is implicated in OX
2022-04-02
In T cells, whereas SETDB1 is implicated in OX40-dependent repression of the Il17a locus in Th17 cells (Xiao et al., 2016), SUV39H1 controls Th2 cell stability by depositing H3K9me3 at the Ifng promoter (Allan et al., 2012). However, the deregulation of the Ifng locus observed in Suv39h1−/− cells ca
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Describing histone acetylation machinery in rivulus will pro
2022-04-02
Describing histone acetylation machinery in rivulus will provide a basis for understanding the role of epigenetic mechanisms in mediating phenotypic variation, by guiding both phenotypic flexibility in adults and developmental plasticity in young. Together with its biological characteristics, rivulu
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br Main Text Metabolism drives diverse
2022-04-02
Main Text Metabolism drives diverse biological processes including differentiation, proliferation, and effector function in diverse cell types. In particular, the process of mounting an innate immune response to pathogens entails rapid sensing of a wide range of patterns displayed by invading mic
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In tumor cells HK II induction
2022-04-02
In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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Finally worth of mention are few papers
2022-04-02
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a ACET library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series of HO-
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Finally worth of mention are few papers
2022-04-02
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Bezafibrate library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series
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br Disclosure statement br Introduction Nitro phenylethane i
2022-04-02
Disclosure statement Introduction 1-Nitro-2-phenylethane is the first nitro compound isolated from plants [1]. It is a volatile compound found in the essential oil of various species, and its presence provides a pleasant odor that resembles the cinnamon scent [2]. The biogenesis of 1-nitro-2-p
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