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Previous studies have demonstrated that synaptic AMPARs can
2024-07-31

Previous studies have demonstrated that synaptic AMPARs can differ greatly in their mobility; some rapidly and constitutively Aminoallyl-UTP sale in and out of the synaptic membrane, while others remain somewhat stable in the synaptic membrane (Luscher et al., 1999, Luthi et al., 1999). We find that
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Further examination of these vmat IR cells shows that they
2024-07-30

Further examination of these vmat-IR cells shows that they are also positive for vimentin (vim-IR) (Fig. 3A). However, within any one cell there may be a region of weaker vmat-IR, suggesting sub-cellular localization. As also shown in Fig. 3B and C not all vim-IR cells are vmat-IR suggesting that th
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Since non lipoprotein derived free cholesterol is recycled
2024-07-30

Since non-lipoprotein-derived free cholesterol is recycled from the plasma membrane through the endosomal system through receptor-independent mechanisms, we wanted to determine whether ABCA2 could alter the trafficking of this source of free cholesterol. Our approach was to measure the effect of mob
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86 5 synthesis Skeletal pain associated with bone fracture i
2024-07-30

Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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BI-847325 In addition to pH regulation by ion
2024-07-30

In addition to pH regulation by ion (counter-) fluxes, acidification is regulated by the abundance of V-ATPase on organelles, by the pumping activity of the complex and by proton leakage. In yeast, the V-ATPase VO subunit a is the only subunit expressed in two isoforms termed Stv1p and Vph1p. V-ATPa
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br Experimental Procedures Additional information can be fou
2024-07-30

Experimental Procedures Additional information can be found in Supplemental Experimental Procedures. Author Contributions Acknowledgments We thank all members of Lab of Health Chemistry for helpful discussions. This work was supported by Grant-in-Aid for Scientific Research (KAKENHI) from
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Apelin is a peptide hormone
2024-07-30

Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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Expression of Twist and the AR are increased by
2024-07-29

Expression of Twist1 and the AR are increased by oxidative stress, but the change in the receptor (mRNA/protein) is lost after treatment with siRNAs that target Twist 1 (Shiota et al., 2010). Twist 1 was found to bind to E-boxes, 5′-CANNTG-3′, in the proximal promoter (−442 to +51 bp) and upstream r
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br Material and methods br Results Table shows that
2024-07-29

Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),
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br Experimental section br Results and discussion br Conclus
2024-07-29

Experimental section Results and discussion Conclusion Acknowledgement This work was supported by the National Natural Science Foundation of China (Grant Nos. 81401489), the Shanghai Pujiang Program (17PJ1402800) and the Shanghai Sailing Program (Grant No. 14YF1409000). Introduction
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Heart failure is a chronic syndrome
2024-07-29

Heart failure is a chronic syndrome in which the heart is unable of pumping an adequate supply of blood to meet the metabolic requirements of the body or generating the required elevated ventricular filling pressures to maintain output [34]. Despite considerable advances in the treatment of heart fa
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The excellent potencies selectivities and improved PK associ
2024-07-29

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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NLX a k a F or befiradol exhibits nanomolar
2024-07-29

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in colorimetric sale to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally,
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Ten strains of lactobacilli TMW isogenic with strain
2024-07-29

Ten strains of lactobacilli: TMW 1.1434 (isogenic with strain F19 ), TMW 1.1733 (isolated from fermented food), TMW 1.1628 (isolated from baby feces), TMW 1.1609 (isolated from baby feces), TMW 1.1734 (isolated from fermented food), TMW 1.313 (isolated from non-pasteurized Heineken beer), TMW
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As a continuation of our search for a selective
2024-07-29

As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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