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Acknowledgments We acknowledge the Danish
2021-05-22

Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
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The in vivo IC M
2021-05-22

The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free triapin
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Studies on the external dehydrogenases of N crassa have show
2021-05-22

Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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Midazolam oral clearance is used for characterization of
2021-05-22

Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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Lipolysis and fatty acid oxidation are two
2021-05-22

Lipolysis and fatty Oxaliplatin oxidation are two important mechanisms involved in fat reduction. Over stimulation of lipolysis increases the level of FFAs in the serum and causes metabolic perturbation (Koutsari and Jensen, 2006). A large inflow of FFAs to the mitochondria may lead to mitochondria
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We obtained two bands in RT PCR for detection of
2021-05-21

We obtained two bands in RT-PCR for detection of SERPIN1-FOSB fusion when Taq DNA polymerase was used (Fig. 3A). Genuine RT-PCR product of SERPIN1-FOSB fusion was proved to be the shorter one (733 PKI-587 pairs) by sequencing, and the longer band (863 base pairs) was shown to be derived from native
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To develop novel EPAC inhibitors Zhou and co workers
2021-05-21

To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dockin
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We also identified Ubc as a functional E for LNX
2021-05-21

We also identified Ubc13 as a functional E2 for LNX1 and determined the complex structure of LNX1–Ubc13~Ub, which depicts the first step of the ubiquitination process (Fig. 3a.). Comparing structural alignment of the RNF4 RING: Ubc13~Ub: Ube2V2 complex (PDB code 5AIU) [33] and the RNF4:Ubc13~Ub comp
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In all available E E structures the RING
2021-05-21

In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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Introduction Maintenance of genome integrity is essential fo
2021-05-21

Introduction Maintenance of genome integrity is essential for life, and faithful DNA replication and repair ensure this. One of the most important parameters for DNA maintenance is the regulation of optimal concentrations of the four 5′-deoxyribonucleoside-triphosphates (dNTPs) the precursors for D
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Protein expression and purification A mL overnight culture o
2021-05-21

Protein expression and purification. A 3 mL overnight culture of E. coli BL21 (DE3) pLysS pGEX-6P-3-A1S_0222 was grown in Luria-Bertani (LB)-Medium (10 g/L tryptone, 5 g/L yeast extract, 5 g/L NaCl, pH 7.4, 100 μg/mL Amp) at 37 °C and 160 rpm. The overnight culture was diluted 1:100 into 200 mL LB (
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Kuo et al Have shown
2021-05-21

Kuo et al. (2006) Have shown that DAPK1 function in inhibiting microtubule (MT) assembly is through the activation of microtubule affinity-regulating kinases (MARK)/PAR-1 family kinases MARK1/2, which destabilize MT by phosphorylating tau and related MAP2/4. This relation with DAPK1 has demonstrated
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Such concerns do not apply to the anti inflammatory
2021-05-21

Such concerns do not apply to the anti-inflammatory actions shown by the agent, given that CR3465 proved effective in various models of inflammation including guinea pig, rat, and human. Airway inflammation, involving a complex network of local mediators, cytokines, and effector Dehydroandrographol
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For LAU extracted ion chromatograms of the
2021-05-21

For LAU 399, extracted bicuculline chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are show
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Xenobiotic metabolism primarily occurs in liver which contai
2021-05-21

Xenobiotic metabolism primarily occurs in liver, which contains many enzymes to catalyze the transformation of xenobiotic. Usually, cytochrome P-450s (CYP450s) act as the first response for biotransformation of xenobiotic in organisms. CYP450s generally consist of various subfamily enzymes which can
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