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The Lysine mutant is located in the
2019-12-17
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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Interestingly all three lesions that significantly
2019-12-16
Interestingly, all three lesions that significantly inhibited transcription – CPD, εA and the AP site, – promoted insertion of Adenosine Kinase Inhibitor hydrate receptor residues opposite the damaged nucleotide. Thus, bacterial RNAP seems to follow the so-called ‘A-rule’ for incorporation of nucleo
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821 Compound was synthesized by the directed metallation
2019-12-16
Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic 821 by conversion into the acid chlori
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Latrunculin B Carbazole could be recrystallised from ethyl
2019-12-16
Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C1
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The requisite extended benzyl alcohols and and
2019-12-16
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by O-
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br Results and discussion Compounds were tested for their
2019-12-16
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Under conditions of energy scarcity
2019-12-16
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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In the Cu bioassay notwithstanding the absence of significan
2019-12-16
In the Cu bioassay, notwithstanding the absence of significant Cu bioaccumulation in bulk tissues over the 96-h exposure period (less than 2-fold difference in tissue Cu between controls and the second-highest treatment), T-ChE activity increased with Cu concentration in gill and, to a lesser extent
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br Discussion Before comparing our results with structural s
2019-12-16
Discussion Before comparing our results with structural studies, we can turn to the Wiki on transition state theory (1935), which explains the reaction rates of elementary chemical reactions in terms of two parameters in one dimension. Structural studies contain information on the ground state, a
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In light of the overall loss of activity and
2019-12-16
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Soybean Glycine max is an important oilseed and can be
2019-12-16
Soybean (Glycine max) is an important oilseed and can be a useful source of epoxy fatty acids (EFAs). This UFA contains an oxygen bridge across adjacent carbon atoms at single or multiple positions in the acyl chain, making them highly reactive and prone to cross-linking, and thus valuable industria
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br Structure of ketosteroid dehydrogenase
2019-12-16
Structure of 3-ketosteroid Δ1-dehydrogenase Overall fold — High-resolution crystal structures of Δ1-KSTD are currently available for the Δ1-KSTD1 isoenzyme from R. erythropolis SQ1 [30]. The Δ1-KSTD1 molecule has an elongated shape, and consists of two domains, an FAD-binding domain and a catalyt
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During ischemia the impact of CK on mitochondria varies
2019-12-14
During ischemia, the impact of CK2 on mitochondria varies in different organs/tissues. For example, CK2α upregulation during ischemia leads to disrupted mitochondrial homeostasis and mediates cardiomyocyte ischemic injury [31]. Specifically, ischemia/reperfusion (I/R) progressively increases CK2α to
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A widely accepted mechanism to
2019-12-14
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the Timolol Maleate [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pivotal for
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The presence of a vicious cycle established between tumor pr
2019-12-14
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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