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N Cyclopentylmethyl analog exhibited fold less potent recept
2020-12-28
N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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The acid base properties of the IL
2020-12-28
3. The acid-base properties of the IL are important issues to consider because protonation changes caused by Brønsted-acidic or basic ions may result in enzyme deactivation [29]. Thereby, the acid-base properties of the newly designed IL need proper control for enzymes by selection of appropriate ca
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Whichever interactions are formed between the DS domains and
2020-12-28
Whichever interactions are formed between the DS domains and the collagen ligand, they are expected to lead to structural changes within the DDR dimer that are propagated across the cell membrane to result in DDR autophosphorylation (Noordeen et al., 2006). Tight coupling of the extracellular confor
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It is particularly notable that CYP
2020-12-28
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 JNJ-10198409 synthesis in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time an
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In essential hypertensive patients it
2020-12-28
In essential hypertensive patients, it is known that the CB is enlarged (Habeck, 1986). In addition to morphological changes in the CB, hyperventilation was reported in essential hypertensive patients at resting conditions (Trzebski et al., 1982). Furthermore, CB is innervated by postganglionic symp
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br Conclusion Determining whether the multiple
2020-12-28
Conclusion Determining whether the multiple putative algal DGAT isoforms are functional DGATs via biochemical assays will be vital in our effort to genetically engineer algae to produce TAG on a large enough scale to make biodiesel production viable. As can be seen in O. tauri, it is possible tha
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br Cytokines as targets for the
2020-12-28
Cytokines as targets for the development of drugs Since the first scientific evidence describing the large number of cytokines and their functional roles and involvement in molecular mechanism of various diseases or disorders researchers have targeted cytokines. (Isaacs and Lindenmann, 1957), Des
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2189 br Results br Discussion br Conclusions br Acknowledgme
2020-12-28
Results Discussion Conclusions Acknowledgments The basic studies were funded in part by a grant of the Clinical Research, Endocrinology and Metabolism Merck Research Laboratories, Medical School Grant Committee for Ezetimibe, Rahway, NJ, USA. Introduction Elevated cholesterol, partic
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br Discussion br Conflicts of interest br
2020-12-28
Discussion Conflicts of interest Acknowledgment Introduction Ewing's sarcoma (EWS) is a bone cancer arising mostly in children. In 1921, EWS was originally described as “diffuse endothelioma of bone” by Dr. James R. Ewing, an American pathologist [1]. In 1992, Ewing sarcoma breakpoint re
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The same reservoir of genes
2020-12-28
The same reservoir of BAPTA-AM sale is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonable. For
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br EphB as a therapeutic target in cancer Eph receptors
2020-12-28
EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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br Enzyme catalysis A biochemically
2020-12-26
Enzyme catalysis A biochemically spontaneous process proceeds in a direction where free Exo1 of the system decreases. However, every spontaneous or energetically favorable reaction needs to overcome an energy barrier known as the activation energy barrier because of the formation of an unstable t
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PF 4800567 hydrochloride In mammals neutrophil elastase is a
2020-12-26
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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The chemical structures of I C MOI and MI
2020-12-26
The chemical structures of I3C, 3MOI, and 3MI and the adenosine monophosphate responsible for 3MI metabolism in rainbow trout and carp are shown in Fig. 4. Discussion To determine the individual CYP450 isoforms involved in 3MI metabolism, we used specific inhibitors for CYP1A, CYP3A and CYP2E1.
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br Results br Discussion PKR
2020-12-25
Results Discussion PKR is activated by viral dsRNA and exerts its antiviral effect through phosphorylation of eIF2a. Because eIF2a phosphorylation leads to attenuation of protein synthesis, many viruses have evolved mechanisms to block or suppress PKR activation. Some viruses use alternative t
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