• summarizes FAAH inhibition data for a series of benzofuran

  2022-03-26

  

  summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio

• Poly (A) Tailing br What are the local exocytotic protein ta

  2022-03-26

  

  What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],

• In an effort to more fully

  2022-03-26

  

  In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold

• With the aim to identify potential novel targets in

  2022-03-26

  

  With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum

• In C elegans KDM A appears to

  2022-03-26

  

  In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene

• MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl

  2022-03-26

  

  MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr

• In the adult normal spinal cord the

  2022-03-26

  

  In the adult normal spinal cord, the resident cells mainly include neurons, astrocytes, oligodendroglia and microglia (Lecca et al., 2012, Miyagi et al., 2012). After SCI, the lesion microenvironment is complex, which includes the functional changes of CNS resident cells and the infiltration of leuk

• VDAC interacts with hexokinase and is implicated in NLRP act

  2022-03-26

  

  VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function

• It has been demonstrated that HO inhibits the production

  2022-03-26

  

  It has been demonstrated that HO-1 inhibits the production of proinflammatory mediators including TNF-α and IL-6 in response to sepsis [35], and the expression of iNOS and COX-2 [36,37]. An inverse association between HO-1 and iNOS has previously been described: the NO levels decline with increases

• HOs can be found in both plants

  2022-03-26

  

  HOs can be found in both plants and animals and they are evolutionarily conserved proteins [8]. There are two HO isoenzymes: inducible heme oxygenase-1 (HO-1) and constitutive heme oxygenase-2 (HO-2) encoded by different genes [9,10]. Biosynthesis of a stress-inducible HO-1 can be triggered by a var

• The isoenzyme hGSTP is an attractive drug

  2022-03-25

  

  The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t

• br Experimental br Acknowledgments The authors are grateful

  2022-03-25

  

  Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve

• Introduction GPR is a class A

  2022-03-25

  

  Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L Riboflavin of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-1 (GLP-1) in the intest

• Recently higher grade varicoceles have been reported to be a

  2022-03-25

  

  Recently, higher-grade varicoceles have been reported to be associated with higher nocturia levels [20], and we observed an interesting phenomenon in which the urine volume/water intake ratio dramatically increased in the rat model of experimental left varicocele (ELV); the decreases in hypothalamic

• k j and d were then submitted to

  2022-03-25

  

  15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil

14296 records 458/954 page Previous Next First page 上5页 456457458459460 下5页 Last page