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For some agonists these stable GPR
2021-09-24
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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pka inhibitor br Regulation of Glu transporters The
2021-09-24
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino pka inhibitor calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transc
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flt3 inhibitor In addition to GABA mediated mIPSCs glutamate
2021-09-24
In addition to GABA-mediated mIPSCs, glutamate-mediated miniature excitatory postsynaptic potentials (mEPSCs) regulate the excitability of the nervous system. GluRs can be divided into ionic and metabotropic GluRs. Ionotropic GluRs can be pharmacologically differentiated by specific binding of the a
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Ionotropic glutamate receptors GluRs are ligand gated
2021-09-24
Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio
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br Experimental section br Acknowledgments MIN cells were ki
2021-09-24
Experimental section Acknowledgments MIN6 ampk pathway were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H06574 to T.U.)
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Gastric inhibitory polypeptide a hormone belonging to
2021-09-24
Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression
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Extending time action is another strategy to increase
2021-09-24
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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br Methods br Results br Discussion In this
2021-09-24
Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig
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br Acknowledgements We thank the following individuals for
2021-09-24
Acknowledgements We thank the following individuals for notable contributions to this work: Dr. Ruth Wood, Dr. Alan Watts, Dr. Casey Donovan, Andrea Suarez, Emily Nakamoto, Allison Apfel, April Banayan, and Jonathan Cheung. This study was supported by the National Institute of Health grants, DK10
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The canonical tumor suppressor p has also been implicated
2021-09-24
The canonical tumor suppressor p53 has also been implicated as a transcriptional mediator of ferroptotic death (Jiang et al., 2015, Tarangelo et al., 2018, Wang et al., 2016, Xie et al., 2017). Specifically, p53 negatively regulates transcription of SLC7A11, the cystine-glutamate antiporter (Xc-) (J
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A breakthrough in the understanding of the
2021-09-24
A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty Kobe0065 synthesis metabolizing enzyme [92], in the execution of GPX4-kn
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PF-5274857 Andexanet alfa works as a decoy for
2021-09-24
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Consideration must be given to both
2021-09-23
Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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Substitutions V L F V and Q H were identified
2021-09-23
Substitutions V36L, F43V and Q80H were identified in the present study. RAS V36L is associated with resistance to boceprevir [18]. In 2015, Brazilian clinical practice guidelines on the management of hepatitis C no longer included combined therapies with boceprevir or telaprevir as a treatment optio
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On the basis of the structure of the
2021-09-23
On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a Alfacalcidol sale with Asp756 in ACAP2, while the methyl group is
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