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Congenital Gcgr mice exhibit increased hepatic Fgf expressio
2022-04-18

Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific Linifanib impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405319 lowe
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Given the actions of GIP analogues administered as a single
2022-04-18

Given the actions of GIP analogues administered as a single dose to ob/ob mice, studies were performed to assess their ability to act in vivo as antagonists of GIP-induced insulinotropic and antihyperglycaemic actions. (Ala3)GIP, (Phe3)GIP, (Tyr3)GIP and (Pro3)GIP all counteracted the glucose-loweri
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ion channel br Materials and methods br
2022-04-18

Materials and methods Results Discussion Employment of GIPR signaling, specifically the direction of this manipulation, as a strategy to improve body weight remains a contentious subject of intense scientific investigation [22], [32], [33]. Despite the physiological benefits of GIP on ion c
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The atomic model of Ce INX provides an additional interpreta
2022-04-18

The atomic model of Ce-INX6 provides an additional interpretation to the Ce-INX6ΔN mutant structure at low-resolution [41]. Given that the N-terminal residues from 2 to 19 are deleted in the Ce-INX6ΔN mutant, the N-terminal funnel found in the pore of the wild-type Ce-INX6 should be lost in the Ce-I
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In a follow up study the
2022-04-18

In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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Recently Bristol Myers Squibb and
2022-04-18

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic 412 2 derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists with
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br Acknowledgement The authors would like
2022-04-16

Acknowledgement The authors would like to thank the University of Johannesburg and the National Research Foundation for the financial support. Mr. D Harris and Dr. R Meyer from Shimadzu South Africa are thanked for their technical support. Prof Ian Dubery is thanked for access to the LC-MS instru
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Signaling pathways such as BMP FGF
2022-04-16

Signaling pathways such as BMP, FGF, and WNT are strongly involved in the process of endochondral ossification and Meckel's cartilage development [20]. Interestingly, absence of BMP antagonist, Noggin, in Meckel's cartilage, resulted in a phenotype, very similar to that of Setdb1 CKO [16]. To examin
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Benzene metabolism occurs primarily in the liver
2022-04-16

Benzene metabolism occurs primarily in the liver where benzene is converted into phenol, catechol, hydroquinone (HQ). HQ is further converted to 1,4-benzoquinone (1,4-BQ) in the bone marrow which is the primary organ of benzene toxicity (Bolton et al., 2000). 1,4-BQ is an important benzene metabolit
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br Conflict of interest br Funding
2022-04-16

Conflict of interest Funding Introduction Heme is an essential molecule for cellular metabolism involving oxygen and electron transfer [1]. However, free heme is a potent pro-oxidant that catalyzes the generation of reactive oxygen species (ROS) leading to cellular damage [2]. Heme oxygenas
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neuraminidase inhibitors More recently Vismodegib was admini
2022-04-16

More recently, Vismodegib was administered in combination with Gemcitabine in a pilot clinical trial that enrolled 23 patients affected by metastatic pancreatic adenocarcinoma. This type of malignancy is the most frequent form of pancreas cancer and is ranked in fourth place for cancer mortality in
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Biological evaluations of the compounds
2022-04-16

Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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br Materials and methods br Results br Discussion Directly
2022-04-16

Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic sigma 1 receptor is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer.
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At days and hours after MI the
2022-04-16

At 21 days and 24 hours after MI, the protein expressions of active JNK1 (P pgc-1α inhibitor of p38 was down-regulated only at 21 days after MI (P Discussion This study demonstrates the role of GSTP1 in HF by inhibiting the TRAF2-induced MAPK activation and the potent inhibitory effect of GSTP1
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Also the decrease in adipocyte cAMP levels
2022-04-16

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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