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Of the acidic hydroxyazoles involved hydroxypyrazole had
2019-12-12
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Multiple sequence alignment of the proteins in
2019-12-12
Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino tetracaine hydrochloride residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found
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The crystal structure of the B subtilis Maf BSU
2019-12-12
The crystal structure of the B. subtilis Maf (BSU28050) was published in 2000, and, to date, it represents the only experimental work with a purified Maf protein (Minasov et al., 2000). The structure revealed a structural fold similar to that found in ITPases and YjjX proteins, which are nucleotide
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In this study we further investigated the involvement of
2019-12-12
In this study, we further investigated the involvement of CRF1 and CRF2 receptors of the dPAG in the regulation of panic-related responses. For this, we used two animal models that associate escape behavior with panic attacks: the elevated T maze and the electrical stimulation of the dPAG (for a ful
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DIG-11-dUTP synthesis AMPK is a master regulator of metaboli
2019-12-12
AMPK is a master regulator of metabolic homeostasis, its broad spectrum of metabolic activities makes it an attractive target for treatment of metabolic and related disorders including Diabetes and Obesity (Madhavi et al., 2018). It controls lipid metabolism through its target genes PPAR-γ, C/EBP-α
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Conventional configurations for alkanolamine and
2019-12-12
Conventional configurations for alkanolamine and A-71623 australia gas are not suitable to represent the chemical reaction between acid gas and alkanolamines. Nevertheless, Dowell et al. [17] have successfully represented the phase behaviour of CO2-water-MEA systems by using SAFT-VR [18] without an
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PF-06447475 sale Acknowledgments The authors thank Dr Vladim
2019-12-12
Acknowledgments The authors thank Dr. Vladimir Poltoratsky and Zhihui Xiao for their help with the in vitro FRET assay. Support for this research was provided by Saint John’s University. Introduction We predicted the existence of endothelium-derived contractile factors (EDCFs) in 1982 [1]. In 1
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actin polymerization inhibitor As illustrated in Table monoc
2019-12-12
As illustrated in Table 3, monocyclic actin polymerization inhibitor analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9
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A major open question in
2019-12-12
A major open question in the field of lipid mediators is the molecular nature of the PLA2 enzyme involved in the release of DHA and related omega-3 fatty acids from phospholipids as a first committed step for the generation of SPMs. Although by analogy with AA it is often assumed that cPLA2α may ser
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In summary synthetic routes with
2019-12-12
In summary, synthetic routes with moderate to high yields have been developed to produce difluoro-dioxolo-benzoimidazol-benzamides including reference standards and , and -desmethylated precursors and , and carbon-11-labeled difluoro-dioxolo-benzoimidazol-benzamides target tracers [C] and [C]. The
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Studies have recently raised concerns about
2019-12-11
Studies have recently raised concerns about the potential role of parabens in breast cancer, as these chemicals are commonly detectable in human breast cancer tissues. An analysis of 160 breast tissue samples collected from 40 mastectomies for primary breast cancer in England showed that at least on
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In our former work our interest was in discovery of
2019-12-11
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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TKI discontinuation studies demonstrate that a portion
2019-12-11
TKI discontinuation studies demonstrate that a portion of TKI-treated CML patients remain in remission for up to 3 years, although long-term risk assessment is still necessary (Bansal and Radich, 2016). The majority of CML patients depend on lifetime TKI treatment, and substantial efforts have been
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br Ultrasonic pretreatment of substrates Substrate pretreatm
2019-12-11
Ultrasonic pretreatment of substrates Substrate pretreatment is widely used in the biofuel, textile and food industries since the substrates are always difficult to degrade. During some enzymatic hydrolysis reactions, the protective layer of the substrate impedes the reaction. Ultrasonic treatmen
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Cy5 EGFP mRNA Herein the interactions of etamicastat nepicas
2019-12-11
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 Cy5 EGFP mRNA exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of BCRP re
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