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The potent estrogen EE induced a decrease in
2019-12-26
The potent Mycophenolate Mofetil EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who exp
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The in vitro enantioselective metabolism of pesticides has b
2019-12-26
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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protein kinase ER stress was monitored by both an increase o
2019-12-26
ER stress was monitored by both an increase of the ER chaperone (GRP78, GRP94) and the activation of the ER resident caspase-12. ER stress response (also known as the unfolded protein response) is a defense mechanism against various cellular stresses which causes accumulation of unfolded proteins in
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Bezafibrate br Acknowledgements The study of RING
2019-12-26
Acknowledgements The study of RING-type E3s continues to grow extremely rapidly. We regret that it was possible to only cite a fraction of the outstanding primary publications in this field. This work was supported by the National Institute of General Medical Sciences grants R01 GM088055 and R01
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HCV has evolved mechanisms to
2019-12-26
HCV has evolved mechanisms to evade humoral immune responses including high functional flexibility and variability of immunogenic portions of its envelope proteins. The highest sequence variability occurs in the first 27 ghrelin receptor of the N-terminus of E2, which is referred to as the hypervari
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The interface between the E ligase and the E enzyme
2019-12-26
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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br Results br Discussion In this
2019-12-26
Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Mithramycin A sale via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-
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Our recent discovery M P H R A S of
2019-12-26
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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br Funding This work was supported by grants to
2019-12-26
Funding This work was supported by grants to A.S. from the Swedish Cancer Foundation, Sweden (Grant number: CAN, 2015/637), the Swedish Medical Council, Sweden (Grant number: 2017- 01274), the Foundations at Skåne University Hospital, Sweden and to KB, SRS, NC, BCS, and SS from the Royal Physiogr
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br Results br Discussion Unraveling the molecular details
2019-12-26
Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr
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69 7 synthesis The discoidin domain receptors DDR and DDR ar
2019-12-24
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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br Materials and methods br Acknowledgments br Introduction
2019-12-24
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the 2-Amino-ATP of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The simplest of the
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Findings from this study also indicate that DAPK regulated
2019-12-24
Findings from this study also indicate that DAPK regulated BimEL expression during OGD as DAPK shRNA transfection inhibited OGD-induced increase of BimEL. A previous study shows that Bim is found in ER compartment in stressed Cerdulatinib receptor but not in normal cells, indicating translocation o
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In general terms PLA s participate in the Lands cycle
2019-12-24
In general terms, PLA2s participate in the Lands cycle of phospholipid fatty Azimilide recycling [1,15,25], whereby the fatty acid composition at the sn-2 position of phospholipids is tightly controlled by a balance between hydrolytic reactions mediated by PLA2s versus activation of the free fatty
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It has been reported that the ECD of DDRs require
2019-12-24
It has been reported that the ECD of DDRs require dimerization and/or oligomerization for binding to collagen.,, Here, we have established using SPR that antibody-mediated oligomerization of DDR2-Fc significantly enhances its binding to immobilized collagen type 1. Our results are consistent with ea
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