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Since OH PGE is a moderately selective EP
2021-06-04
Since 1-OH-PGE2 is a moderately selective EP4 agonist which could bind to mouse EP3 and EP4 with a relatively similar affinity (Kiriyama et al., 1997), we have used a highly selective EP4 agonist CAY10580 to evaluate the involvement of EP4 activation in PGE2-facilitated EP4 internalization and recyc
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br Introduction Hydrogen sulfide H S and
2021-06-04
Introduction Hydrogen sulfide (H2S) and nitric oxide (NO) are important gasotransmitters in the cardiovascular system and instrumental to the fine control of vascular tone [1] and cellular function [2]. NO is synthesized from l-arginine by calmodulin-dependent endothelial nitric oxide synthase (e
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A structural explanation for how RBR RING s
2021-06-04
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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br Results and discussion br Conclusion We
2021-06-04
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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br Conclusion The present work describes the
2021-06-04
Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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br DGAT protein interactions Although DGAT
2021-06-04
DGAT-protein interactions Although DGAT1 and DGAT2 are membrane proteins of the ER, the ER contains within its extensive three-dimensional network different, unique structural and functional protein domains that arise from the non-uniformity imposed on it by the intracellular structures it intera
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Moreover the vibrational contributions provide a plausible
2021-06-03
Moreover, the vibrational contributions provide a plausible explanation for the missing X′ peaks in the experimental PES for the Er and Tm complexes. The current SO-MCQDPT2 (Fig. 1(k) and (l)) and MCQDPT2 II (Fig. 2(k) and (l)) calculations suggest the appearance of peak splittings for these complex
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TNF-alpha, recombinant murine protein australia Synthetic pr
2021-06-03
Synthetic progestogens (also known as ‘synthetic gestagens’, ‘synthetic progestins’ or simply ‘progestins’) are designed to mimic the effects of progesterone (P4) and are the active pharmaceutical ingredient in many contraceptives and hormone replacement therapies. Since most progestins are derived
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br Acknowledgements br Introduction Ischemic retinopathy is
2021-06-03
Acknowledgements Introduction Ischemic retinopathy is common to the major causes of blindness, including proliferative diabetic retinopathy, venous occlusion, and retinopathy of prematurity. The hypoxia that follows retinal capillary obliteration drives deregulated growth of new blood vessels
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CX-6258 synthesis br Methods Ventricular cardiomyocytes from
2021-06-03
Methods Ventricular cardiomyocytes from adult male Wistar rats were isolated using a standard enzymatic digestion [11]. Cells were incubated at 37°C for 4 to 6h with Tyrode solution (in mM: 140 NaCl, 4 KCl, 1.1 MgCl2, 10 HEPES, 10 glucose, 1.8 CaCl2; pH7.4, with NaOH) supplemented or not with 10μ
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As a co factor CIITA
2021-06-03
As a co-factor, CIITA lacks the ability to recognize and directly bind to specific DNA elements to regulate transcription; instead, it relies on interaction with sequence-specific transcription factors (TFs) to be recruited to the chromatin. Therefore, the observation that CIITA binds to a specific
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br Acknowledgements br Introduction Endothelial cells consti
2021-06-03
Acknowledgements Introduction Endothelial thymidylate synthase constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile
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br Introduction Epidermal growth factor receptor EGFR activa
2021-06-03
Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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The lack of robust immunocompetent
2021-06-03
The lack of robust immunocompetent animal models permissive for HCV makes it hard to assess if the quantity and quality of vaccine-induced immunity is sufficient to confer protection. Thus, it is difficult to predict to what extent antibody responses induced by current vaccination approaches, includ
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The focus of this review is on
2021-06-02
The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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