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Paxilline br Oxidoreductase like MEM for
2020-06-30
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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ER redox imbalance leads to the accumulation of misfolded pr
2020-06-30
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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A growing number of other post translational modifications
2020-06-30
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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BIBR-1048 br Experimental section br Author contributions br
2020-06-30
Experimental section Author contributions Acknowledgements Introduction Many BIBR-1048 in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-cata
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Conversely to the reduction in restraint evoked HR increase
2020-06-30
Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF Cy5.5 hydrazide sale antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, these resu
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It is currently believed that acute
2020-06-29
It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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The outcome of DGK function will thus depend
2020-06-29
The outcome of DGK function will thus depend on the binding partners of each DGK isoform, and the effects that they exert can be quite different. A clear example of this concept has been demonstrated for the type IV DGKs, ζ and ι, which are structurally very similar but have opposing effects on Ras
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br Funding br Conflict of
2020-06-29
Funding Conflict of interests Introduction DAG is generated by the hydrolysis of phosphatidylinositol-4,5-bisphosphate (PtdIns(4,5)P2) by PtdIns-specific phospholipase C (PLC) enzymes [1]. Remaining in the membrane, it binds proteins with cysteine-rich, C1 domains, and activates several of
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In children only the genotype was associated with spina bifi
2020-06-29
In children, only the 6/7 genotype was associated with spina bifida, increasing the risk about 4 times relative to the DHFR 3/3 and 6/6 genotypes. However, the 95%CIs are broad and only few spina bifida patients have the DHFR 6/7 genotype. The effect of the 6/7 genotype on spina bifida risk is there
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br Conflict of interest statement br Acknowledgement The
2020-06-29
Conflict of interest statement Acknowledgement The study was financially supported by the Ministry of Education, Youth and Sports of the Czech Republic – projects “CENAKVA” (No. CZ.1.05/2.1.00/01.0024) and “CENAKVA II” (No. LO1205 under the NPU I program), by the Grant Agency of the University
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Cytochromes P CYP are a superfamily of hemoproteins containi
2020-06-29
Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xe
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96365 br Pre clinical combination studies using
2020-06-29
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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Kim et al reported for bioactive compounds originating
2020-06-29
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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Accumulated evidence indicates that apelin plays
2020-06-29
Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 ache inhibitor
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Gastrointestinal tone can be effectively modulated by cholin
2020-06-29
Gastrointestinal tone can be effectively modulated by cholinesterase inhibitors. As parasympathetic fibers release PF-2341066 to contract the circular and longitudinal intestinal muscles, AChE inhibition can facilitate those actions. Postoperative ileus (delayed gastric emptying after surgery) can a
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