• br Acknowledgements This study was supported by

  2022-01-11

  

  Acknowledgements This study was supported by National Institutes of Health grant (R01GM104037), VA grant (BX002741), and Rutgers Busch grant. Nuclear receptor FXR is the master regulator of bile acids homeostasis The farnesoid X receptor (FXR) belongs to a family of proteins known as nuclear

• So what makes a FFAR agonist different

  2022-01-11

  

  So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept

• tool The newly synthesized compounds were evaluated

  2022-01-11

  

  The newly synthesized compounds were evaluated for their FAAH inhibitory activity in vitro. In addition, molecular modeling, selectivity and reversibility behavior of the new class of FAAH inhibitors are presented in this article. Results and discussion The potency of inhibition on the human rec

• To validate the effects of the G a HMT inhibitors

  2022-01-11

  

  To validate the effects of the G9a HMT inhibitors on HMEC-1 RG-108 and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression were effectively decreased (Fig

• Cyclopamine a steroidal alkaloid type secondary

  2022-01-11

  

  Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas

• The fibulins are a newly abundantly in

  2022-01-11

  

  The fibulins are a newly abundantly in the basement membrane of blood vessels. Among them, fibulin-1 is essential for elastin polymerization. Tropoelastin cannot be assembled into mature elastin fibrils without the functional fibulin-1. In adult blood vessels, pronounced fibulin 1 deposition can be

• The activation of AKT and ERK results

  2022-01-11

  

  The activation of AKT and ERK1/2 results in the stabilization and increase in the co-transcriptional function of β-catenin [31], [32], [33]. Here, (R,R′)-MNF was found to reduce the levels of phospho-active AKT and ERK, which, in turn, may regulate the abundance and signaling potential of β-catenin.

• Acyclovir It was reported that GPR is expressed on macrophag

  2022-01-11

  

  It was reported that GPR120 is expressed on macrophages in adipose tissue (Oh et al., 2010). Whether GPR120-positive Acyclovir in human and rat pancreas belongs to macrophages was studied. CD68 is a transmembrane glycoprotein that is highly expressed by human monocytes and tissue macrophages (Horika

• br Materials and methods br Results

  2022-01-11

  

  Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited

• Petrat et al could show that even

  2022-01-10

  

  Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c

• br Materials and Methods br

  2022-01-10

  

  Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CTClindamycin HCl receptor was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expr

• br Materials and methods br Results br

  2022-01-10

  

  Materials and methods Results Discussion Here, we investigated the inhibitory effects and associated mechanisms of phloroglucinol on α-glucosidase. Our results showed that phloroglucinol reversibly inhibited α-glucosidase in a dose-dependent manner (Fig. 1), with the double-reciprocal plot

• Formyl peptide receptors FPRs are a family

  2022-01-10

  

  Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on

• Polyunsaturated fatty acids PUFAs represent a class of lipid

  2022-01-10

  

  Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic DASA-58 (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachidonic acid (AA)

• br Introduction More than structurally different isoprenoids

  2022-01-10

  

  Introduction More than 30,000 structurally different isoprenoids, such as steroids, carotenoids, prenyl side-chain of quinones, prenyl proteins, and natural rubber, exist in nature. In a biosynthetic pathway, linear prenyl diphosphates are common structures as a precursor of isoprenoids, as shown

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