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In accordance with its similarity to classical NLSs Importin
2022-04-18

In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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hyPerFUsion™ high-fidelity DNA polymerase br Conflict of int
2022-04-18

Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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In order to address the Cyp inhibition
2022-04-18

In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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The current gold standard for
2022-04-18

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) indocid sale (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid an
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Evidence demonstrating the interplay between hypoxia and the
2022-04-16

Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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A biochemical characterisation of this functionally crucial
2022-04-16

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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small molecule library screening br Discussion Our results s
2022-04-16

Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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The following are the supplementary
2022-04-16

The following are the supplementary data related to this article. Transparency document Introduction Hypoxia is a pathological process that causes abnormal changes in metabolism, function and morphological structure of tissue because of insufficient oxygen supply. It's reported that hypoxia w
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Long term effects of prolonged
2022-04-16

Long-term effects of prolonged darkness on specific physiological activities were also monitored at different leaf positions. Basically, stomatal conductance and CO2 assimilation were different at various leaf stages and were decreased or inhibited significantly within 24 h in all leaf positions upo
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CD CD belong to the costimulatory adhesion molecule family w
2022-04-16

CD80/CD86 belong to the costimulatory adhesion molecule family, which can activate T scd1 by the costimulatory pathway and have been used as indicators of DC maturation in numerous studies. In addition, MHC-II, as the principal component of antigen presentation, was significantly elevated after ant
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br Trifluoromethylketones This group of compounds was demons
2022-04-16

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc IMD 0354 in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif for
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Camptothecin is a type of topo I inhibitor and its
2022-04-16

Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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In the course of studies leading to the discovery
2022-04-16

In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Under increased drug pressure more protease variants with mo
2022-04-16

Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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There is evidence for an
2022-04-16

There is evidence for an adverse sympatho-stimulatory effect in the medulla oblongata mediated by the α1/β1 isoform, implying a possible benefit of selective α2/β1 activation [19]. While the stimulator BAY 41–2272 increases NO-sensitivity of both isoforms [20], a prevalence of the α1/β1 isoform comp
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