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ERAP has been crystallized in two different conformations wh
2023-09-07

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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In summary our data have shown that one mechanism
2023-09-07

In summary, our data have shown that one mechanism by which glucose may mediate monocyte–endothelial cell interaction in the retinal endothelial cells is via the 12/15-LO pathway Furthermore, our current and previously published data [20,22] indicate a differential role of endothelial 12/15-LO versu
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The putative physiological meaning of epinephrine related he
2023-09-07

The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c
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Given these findings above we hypothesized that hypernocicep
2023-09-07

Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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An alternative approach to the administration
2023-09-07

An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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A high throughput small molecule ACK biochemical
2023-09-07

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Calcitriol to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was p
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By promoting bundling and processive elongation of actin fil
2023-09-07

By promoting bundling and processive elongation of DDD107498 filaments and inhibiting association of capping protein with filament barbed ends, Ena/VASP family proteins contribute to the dynamics of lamellipodia and filopodia [41] and maintenance of focal adhesions and tight junctions [42, 43]. Acc
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Based on the improved characteristics of the mutant ECDs
2023-09-07

Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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br Acknowledgments We thank the anonymous reviewers
2023-09-07

Acknowledgments We thank the anonymous reviewers for their constructive comments on the manuscript, and also thank Dr. Hans-U. Dahms for his comments on the manuscript. This work was supported by a grant from the National Research Foundation (2009-0071218) funded to Young-Mi Lee. This work was al
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Recent studies have demonstrated that in response
2023-09-06

Recent studies have demonstrated that in response to IR, hundreds of substrates are phosphorylated in an ATM-dependent manner, clearly demonstrating the complexity of the ATM-mediated DDR pathways (Matsuoka et al., 2007, Bennetzen et al., 2010, Bensimon et al., 2010). However, evidence suggesting th
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br Apelin The APJ receptor ligand apelin firstly
2023-09-06

Apelin The APJ receptor ligand apelin firstly in 1998 was segregated from bovine stomach tissue. Human preproapelin gene located on chromosome Xq25–26.1. The apelin preproproteins consist of 77 amino lumiracoxib residues that are cleaved into biologically active C-terminal fragments of various s
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The first identified auxiliary subunit
2023-09-06

The first identified auxiliary subunit, stargazin, is essential for AMPAR function in cerebellar granule neurons (Hashimoto et al., 1999). Subsequently, a family of six transmembrane AMPAR regulatory proteins (TARPs) were defined that modify channel trafficking, gating, and pharmacology (Kato and Br
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salubrinal br Results br Discussion Tapinarof GSK
2023-09-06

Results Discussion Tapinarof (GSK2894512) is a naturally derived investigational topical medicine with demonstrated clinical efficacy for patients with AD and psoriasis (Bissonnette et al., 2010, Bissonnette et al., 2012a). The drug substance is a polyphenol produced by bacteria that is struct
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In our study the expression
2023-09-06

In our study, the expression levels of adiponectin and its receptors in the uteri, conceptuses, and throphoblasts were determined by the stage of early pregnancy. Therefore, it could be hypothesized that the adiponectin system is regulated by the local hormonal milieu. Hormonal regulation in the ute
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The present work has implications
2023-09-06

The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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