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PBI is an agonist of GPR and acts as an
2021-09-24

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Material and methods br Results Consistent with our previ
2021-09-24

Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing ANP (1-11), rat in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the membra
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br Acknowledgments br Free fatty acids FFAs are
2021-09-24

Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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br Acknowledgements This work was supported
2021-09-24

Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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There are human genes in
2021-09-24

There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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GK allosteric activators validate the
2021-09-24

GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many
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br Acknowledgments We would like to acknowledge Jenna
2021-09-24

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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Newt GHS R a proteins
2021-09-24

Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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Our previous study had shown that silencing
2021-09-24

Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β FG4592 [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved in the anti-lipo
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Introduction Terpenoids also known as isoprenoids constitute
2021-09-24

Introduction Terpenoids, also known as isoprenoids, constitute a large family of natural products comprising at least 22,000 compounds and play diverse and important roles in plants as hormones, phytosynthetic pigments, and electron carriers [1], [2]. In addition, volatilized terpenoids contribute
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One of the possibilities of HO
2021-09-23

One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing Tranexamic Acid but also have very l
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Importantly HDACi mediated effects are cell
2021-09-23

Importantly, HDACi-mediated effects are cell and HDAC specific; different effects and outcomes have been observed in different cell types, targeting different HDAC isoforms. While HDACi exhibit a strong proapoptotic potential in human leukemia Hydrocortisone 19, 20, 21, 22, they have a limited abil
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These inhibitors possess a cap group build from cyclization
2021-09-23

These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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read the full info here Several compounds have been describe
2021-09-23

Several compounds have been described in the literature as inhibitors of the sGC. Among them, methylene blue and LY83583 () are not direct sGC inhibitors, but rather block cGMP formation by generating superoxide anion radicals that deactivate NO. Despite their extensive use in plethora of research s
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br Materials and methods br Results br Discussion Reduced gl
2021-09-23

Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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