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From an industrial perspective the low turnover numbers and
2021-01-19
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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Emergence of antibiotic resistant strains of Mtb alongwith t
2021-01-19
Emergence of antibiotic resistant strains of Mtb alongwith the inefficacy of widely used Bacillus Calmette-Guerin (BCG) vaccine in adults are major challenges in the treatment and prevention of TB. Elucidation and characterization of new vaccine and drug candidates are therefore required in order to
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Imidazo purine diones were another cluster of compounds iden
2021-01-18
1-Imidazo[2,1-]purine-2,4(3,8)-diones were another cluster of compounds identified from the Chembridge screen (). A benzyl group at the R2 position was preferred over a phenyl or 2-phenylpropyl (. and ), and -substitution of the benzyl group increased potency to the nanomolar level ( IC=0.20μM . ).
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Here we describe a novel
2021-01-18
Here, we describe a novel series of arylazoderivatives developed from CAN508, one of the first known selective CDK9 inhibitors. We focused on modification of both ends of parental molecule, CAN508, in order to improve cytotoxicity and CDK activity. We therefore analyzed how changes in molecules will
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ionomycin Primary renal PNET was first reported by Seemayer
2021-01-18
Primary renal PNET was first reported by Seemayer et al in 1975. The possible etiology of rPNET is based on the theory of neural cell intussusception in the kidney during development that initiates the tumorigenesis. rPNET most commonly affects young adults, with a mean age of 30.4 years and male pr
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br Results and discussion br Conclusions In
2021-01-18
Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of th
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In conclusion our findings suggested that EP receptor activa
2021-01-18
In conclusion, our findings suggested that EP4 receptor activation triggers apoptosis in B-cell lymphoblasts. Our results also showed that EP4 receptor engagement inactivates NF-κB, which, in turn, sensitizes Ramos Desformylflustrabromine hydrochloride to apoptosis induced by chemotherapeutic agents
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There have been reports regarding the use of enolases as
2021-01-18
There have been reports regarding the use of enolases as novel vaccine candidates for A. suum, S. suis, T. pisiformis and T. multiceps on account of this enzyme class's critical role in plasminogen activation and migration across tissue barriers (Chen et al., 2012; Zhang et al., 2009; Zhang et al.,
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br A major physiological action of ET
2021-01-18
A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from en
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br Acknowledgements We would like to thank Dr
2021-01-18
Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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br Expression and Tissue Functions of
2021-01-18
Expression and Tissue Functions of DDRs The DDRs are widely expressed in different tissues, both during development and in adult organisms. DDR1 mRNA is found in many tissues in mice and humans, with high levels in brain, lung, kidney, spleen, and placenta (Di Marco et al., 1993, Johnson et al.,
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In conclusion we demonstrate that infection of salmon cells
2021-01-18
In conclusion we demonstrate that infection of salmon cells with ISAV induce the main branches of the cellular UPR machinery, but also one of its main negative regulators, GADD34. This is probably important for maintaining translation of interferon and interferon stimulated genes (ISGs), keeping ISA
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The concept of GPCRs and EGFRs existing as heteromers
2021-01-18
The concept of GPCRs and EGFRs existing as heteromers is consistent with previous studies. Co-immunoprecipitation studies have shown that agonist stimulation (both AngII and EGF) promotes a multi-protein complex containing the AT1R and EGFR, however these endpoint assays were not in live cells or in
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br In half a century after its first biochemical characteriz
2021-01-18
In 2015–2016, half a century after its first biochemical characterization as a template-independent polymerase, it was shown that TdT can, firstly, assemble a DNA synapsis by itself, optimally with one micro-homology base-pair between strands [] and secondly, perform a template-dependent nucleotid
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MTX and MTXPGs block the activity of
2021-01-18
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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