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We have previously reported DAPK
2021-07-16
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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The three dimensional crystal structure of Ca loaded CaM
2021-07-16
The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo
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In addition we investigated if the previously reported papai
2021-07-16
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time dependen
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Previously the N glycan in V
2021-07-16
Previously, the N-glycan in V3 of HXB2, HXB10, LAI and BRU strains was reported to be dispensable for their infectivity to T cell lines, although detailed growth kinetics and experimental conditions were not described 4, 5, 6, 7, 8. The experiments appear to have been done by infection initiated wit
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In the course of our program which was
2021-07-16
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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In addition to PGC transcriptional co
2021-07-15
In addition to PGC1α, transcriptional co-repressors such as NCOR and RIP140 participate in oxidative muscle remodeling induced by exercise, whereby reductions in their expression and the resulting de-repression of downstream TFs activates oxidative gene expression (Seth et al., 2007, Yamamoto et al.
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Curcumin is found safe in several
2021-07-15
Curcumin is found safe in several human studies (Chainani-Wu, 2003; Cheng et al., 2001; Dcodhar et al., 2013), in contrary, the toxicity of curcumin has also been reported under some specific conditions (Burgos-Morón et al., 2010). Moreover, it Nifedipine was also reported that curcumin induced som
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The optimization of the lead compound
2021-07-15
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic sulconazole moiety with other functional groups led to loss of functional activity against EP4 receptor.
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It is without doubt that the
2021-07-15
It is without doubt that the vagina plays a significant role in the perception of coital stimulation leading to sexual arousal and, finally, orgasm. In response to sensory stimulation, relaxation of vaginal vascular and nonvascular smooth muscle occurs, resulting in an increase in local blood flow a
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br Competing interests br Acknowledgments This work
2021-07-15
Competing interests Acknowledgments This work was supported by grants from Fujian Fujian Provincial Natural Science Foundation (2016J01612). Introduction Cancer is still one of the most serious diseases in the world. According to the World Health Organization (WHO), cancer is the second mo
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At the therapeutic level the logical approach to address
2021-07-15
At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn
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One question relates to our finding
2021-07-15
One question relates to our finding that oxysterol-GPR183 signaling is critical for CP and ILF formation in the colon but dispensable in the small intestine. GPR183 and its ligand were expressed in both the small and large intestines. Moreover, 7α,25-OHC was required for ILC3 migration to CPs not on
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br Materials and Methods br
2021-07-15
Materials and Methods Acknowledgements Authors would like to thank Mr. Pritam Naskar and Mr. Dibya Mukherjee for their help. Authors also acknowledge the help of Mr. Barun Mahata and Dr. Kaushik Biswas, Division of Molecular Medicine, Bose Institute, for human cDNA samples. P.A.B. and A.B.D. w
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The expression of cytokine inducible genes is mediated by
2021-07-15
The expression of cytokine-inducible genes is mediated by a number of components within the cell. It has been shown that Jak2 and the Ras/Raf/MAP kinase signaling cascades are required for the expression of DUB-1[9], [29]. However, the enhancer domain of DUB-1 lacks a consensus sequence for Stat bin
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Acknowledgments We acknowledge the Danish
2021-07-15
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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