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To improve the preferential GalR binding we synthesized M
2021-09-08

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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The GAL also modified HT system
2021-09-08

The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B TAK-875 (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragment
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Albumin is the major carrier of
2021-09-08

Albumin is the major carrier of free fatty acids (FFAs) in plasma [59], and harbours seven binding sites that are common to FFAs with a range of chain-lengths (C10-C18) across its three domains (Fig. 1a) [60,61]. In vitro, saturated, mono- and poly-unsaturated FFAs, with chain lengths ranging from C
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Cy5 TSA Because FPR is expressed in VSMCs and its role
2021-09-08

Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and Cy5 TSA polymerization). First, we tested if FPR-1 is i
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Free Fatty Acid Quantification Colorimetric/Fluorometric Kit
2021-09-08

Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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Glucose induced nuclear translocation of several enzymes inc
2021-09-08

Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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The FAAH inhibitor activity of the ethoxycarbonyl
2021-09-08

The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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NeuroHIV is initiated by HIV crossing the
2021-09-07

NeuroHIV is initiated by HIV crossing the blood–brain barrier (BBB) to enter the CNS. This is thought to occur primarily via the transmigration of infected CD14+CD16+ monocytes (Williams, 2014), using the monocytes as “Trojan Horses” (Peluso, 1985), although some studies suggest alternate routes of
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Antigen presentation of incoming viral particles has been we
2021-09-07

Antigen presentation of incoming viral particles has been well studied for diverse viruses in antigen-presenting cells (APCs), mostly in dendritic cells and macrophages in the context of the exogenous antigens’ pathway to prime the CD8+ T cells. However, CD4+ T cells are not known as efficient APCs,
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harmine receptor br Acknowledgement The authors are
2021-09-07

Acknowledgement The authors are grateful for financial support provided from specific university research (MSMT No 21-SVV/2018). Introduction Several recent studies have demonstrated that planaria, flatworms notable for their regenerative capabilities, can develop conditioned place preference
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In this study we present the first data on
2021-09-07

In this study, we present the first data on the kinetic properties of the hexokinase of T. equiperdum, which we compare with similar data available for pleomorphic T. brucei (Seed and Baquero, 1965, Nwagwu and Opperdoes, 1982, Hara et al., 1997, Morris et al., 2006, Chambers et al., 2008b, Chambers
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roscovitine P Benzoxaborole substituted macrocyclic compound
2021-09-07

P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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Mapping PPI networks is challenging
2021-09-07

Mapping PPI networks is challenging, as it is difficult to express and purify large variaties of rifampicin in sufficient quantities to allow the study of interactions between them. Membrane-bound proteins are particularly difficult to purify in functional form due to their amphiphilic nature. Furt
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In plants NO production is one of the
2021-09-07

In plants, NO production is one of the early responses to stress (Tossi, Lamattina, & Cassia, 2009). Usually, NO signal transduction requires the involvement of downstream signaling compounds. We further investigated the effects of cGMP on GSK-3 expression. The data showed that LY83583 (a cGMP inhib
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In mice iNKT cells are
2021-09-07

In mice, iNKT cells are most frequent (20–30%) among liver T lymphocytes, while they only constitute 0.4–1% of the total T cells in thymus, bone marrow, spleen, lymph node, and intraepithelial lymphocytes. In humans, iNKT cells constitute approximately only a 0.1–0.2% of the peripheral blood T lymph
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