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The Rho family of GTPases is composed of
2021-11-05
The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) Severa
2021-11-05
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) class, (2) analogues with -oriented aryl substituents showed the best inhibition o
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Metal organic frameworks MOFs have
2021-11-05
Metal–organic frameworks (MOFs) have emerged over the past two decades with the potentials to act as promising materials in gas storage, chemical separation, catalyst, magnetism, sensing, and drug delivery etc (Du et al., 2013, Zhou and Kitagawa, 2014). Additionally, the secondary interactions, such
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Under most circumstances NO is a potent endogenous vasodilat
2021-11-04
Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response
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It was noted elsewhere that several of the variants
2021-11-04
It was noted elsewhere that several of the variants (i.e., Indel19 and SNP63) that make up the risk haplotypes had unusually large differences in allele frequencies between Africans and non-Africans, as compared with a set of likely neutral loci (Fullerton et al. 2002). This finding was interpreted
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br Conflict of Interest Both GM
2021-11-04
Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr
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In order to investigate whether this off
2021-11-04
In order to investigate whether this off-target activity was related to a particular structural feature of this CW069 or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups, respectiv
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Ca independent release of L C
2021-11-04
Ca2+-independent release of L-[14C]glutamate and [3Н]GABA that occurs via transporters working in the reverse mode also insignificantly increased in vitamin D3 deficiency despite decreased GAT-3 and EAAC-1 cucurbitacin and neurotransmitter uptake efficacy Fig. 3, Fig. 6 A). However, the upward tend
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Glucose uptake a critical metabolic
2021-11-04
Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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br Conclusions br Acknowledgement Work in the authors
2021-11-04
Conclusions Acknowledgement Work in the authors’ labs was funded by Natural Sciences and Engineering Research Council of Canada (OGP0194652 and OGP0041653) and Diabète Québec. Introduction Fifty years ago, Sydney Brenner proposed Caenorhabditis elegans as a useful model for the study of an
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Recently several studies addressed cytological and biochemic
2021-11-04
Recently, several studies addressed cytological and biochemical features of oocyte aging. It was reported that cytological changes associated with the mammalian post-ovulatory oocyte aging include chromatin disorganization, abnormal meiotic spindle location or its disruption, partial exocytosis of
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ADAM has two alternative splicing
2021-11-04
ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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In conclusion Factor Xa inhibitors edoxaban and rivaroxaban
2021-11-04
In conclusion, Factor Xa inhibitors (edoxaban and rivaroxaban) reduced PVs and SAN spontaneous activities in a concentration-dependent manner. FXa inhibitors may modulate occurrence of atrial fibrillation through PAR1 inhibition and INa-late reduction in PVs. Introduction Enzymes play crucial fu
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Trifluoromethyl ketones and fluorophosphates were the
2021-11-04
Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated
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PKC s effect on quantal size may involve regulation of
2021-11-04
PKC’s effect on quantal size may involve regulation of endocytotic protein components responsible for mediating kiss-and-run exocytosis. There is a growing body of evidence to suggest that canonical endocytotic proteins—dynamin, amphiphysin, syndapin, and others—may play a role in modulating fusion
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