• However the clinical development of

  2022-04-07

  

  However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep

• br Histamine H R Many of the

  2022-04-07

  

  Histamine H3R Many of the highlight H3R ligands have been described as suitable pharmacological tools for in vitro or in vivo studies and are designated here. The number of ligands and structural categories is huge, and a number of inclusive reviews of the SAR and properties of H3R ligands have b

• Racemic protein crystallography has been proven to

  2022-04-06

  

  Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,

• Pharmacologic approaches of inhibiting GSNOR activity have

  2022-04-06

  

  Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications

• siRNA construction and transfection For small interfering RN

  2022-04-06

  

  siRNA construction and transfection. For small interfering RNA (siRNA) experiments, we used Stealth™ select RNAi oligonucleotides targeted against GPR120 (Gibco/Invitrogen). The target sequence of siGPR120 used were; sense 5′-AAGUGGGUGCGAUUGACUUGGUCCA-3′ and antisense 5′-UGGACCAAGUCAAUCGCACCCACUU-3′

• A linker length of and atoms was found to be

  2022-04-06

  

  A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d

• br Materials and methods E coli strains

  2022-04-06

  

  Materials and methods E. coli strains. Strains of E. coli with mutations in the lacZ gene for β-galactosidase [5] and a derivative with a knock-out mutation of the chromosomal gene for FPG produced with P1vir [6] were obtained from H. Schellhorn (McMaster Univ., Hamilton, Ontario, Canada). Growth

• Ketanserin In conclusion atorvastatin but not pravastatin im

  2022-04-06

  

  In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in

• Introduction Human pathogenic Leishmania protozoa comprise d

  2022-04-06

  

  Introduction Human pathogenic Leishmania protozoa comprise 20 different species that are distributed throughout the world and cause the disease leishmaniasis [1]. Transmission primarily occurs through the bite of a female sand fly and clinical manifestations of the disease span from cutaneous lesio

• Although GLP has greater insulin releasing effects at

  2022-04-06

  

  Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts

• The experiments indicate that a major component of the

  2022-04-06

  

  The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in Repaglinide preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in vessels

• These data suggest that the dehydration of the SSRBCs

  2022-04-06

  

  These data suggest that the dehydration of the SSRBCs induced by RANTES might result of an activation of the Gardos channel mediated by the chemokine receptor DARC. However, direct evidence of Gardos channel activation by chemokines in Duffy-positive SSRBCs leading to cell dehydration has not been e

• Chlorhexidine digluconate Sickle erythrocytes are known to h

  2022-04-06

  

  Sickle erythrocytes are known to have an increased adhesion to endothelial Chlorhexidine digluconate (Hebbel et al., 1980, Hebbel et al., 1981a, Hebbel et al., 1981b, Wautier et al., 1985, Mohandas and Evans, 1987). Understanding the events associated with vaso-occlusion requires a detailed knowledg

• In summary two new flexible amine

  2022-04-06

  

  In summary, two new flexible amine-functionalized quinolinium derivatives with far-red region emitting were prepared. The shorter-chain fatty amine side chain in the scaffold of was found to be a more promising G-quadruplex DNA fluorescent probe, suggesting the amine side group plays an important r

• Further our data demonstrate a role for mitochondrial AIF in

  2022-04-02

  

  Further, our data demonstrate a role for mitochondrial AIF in oxidative cell death induced by RSL3. We found that AIF knockdown using siRNA completely protected the nibr against RSL3 induced oxidative stress. Similar to other pathways of caspase-independent programmed cell death, mitochondrial dama

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