• Alogliptin is a potent selective inhibitor of the serine pro

  2020-08-05

  

  Alogliptin is a potent, selective inhibitor of the serine protease DPP-4 [10]. Alogliptin or (2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl] benzonitrile) (C, Fig. 2), a potent (IC50  10,000 over DPP-8 and 9) was identified by replacing the quinazolinone

• The significance of cofilin activation inactivation during a

  2020-08-05

  

  The significance of cofilin activation/inactivation during apoptosis is only poorly understood. To date, there are only few reports showing a role of cofilin in inducing cell death under oxidative stress (Campos et al., 2009, Hsieh et al., 2010, Klamt et al., 2009, Rehklau et al., 2012). Studying th

• Sex also influences COMT effects

  2020-08-05

  

  Sex also influences COMT effects on cognition. Women have 20%–30% less COMT activity than men (Chen et al., 2004, Fahndrich et al., 1980). Both Raz et al. (2011)O\'Hara et al. (2006) found that sex interacted with COMT genotype such that older men who had a Val allele showed greater negative effects

• E ligases have been associated

  2020-08-05

  

  E3 ligases have been associated with a number of pathogenic mechanisms. Mutations in the E3 ligases MDM2, BRCA1, TRIMs, and Parkin have been linked to multiple cancers and neurodegenerative diseases (Fakharzadeh et al., 1991, Hatakeyama, 2011, Welcsh and King, 2001), and MDM2-p53 interaction inhibit

• alpha-Endorphin A range of inhibitors were therefore

  2020-08-04

  

  A range of inhibitors were therefore synthesized containing either carboxylic alpha-Endorphin or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). Ana

• In summary the novel oxadiazole DGAT inhibitor was identifie

  2020-08-04

  

  In summary, the novel oxadiazole DGAT-1 inhibitor was identified and SAR exploitation enabled a design strategy to improve both potency and LLE leading to the clinical candidate , which displayed good pharmacokinetics and demonstrated in vivo efficacy in obesity related models. Results from the fur

• According to the previous experimental investigations the st

  2020-08-04

  

  According to the previous experimental investigations [2,43], the studied ionic liquids shift the P-T equilibrium diagrams of methane hydrate toward higher pressures and lower temperatures, suggesting the inhibitory effects of these Pamidronate Disodium materials on the equilibrium conditions of me

• Another stream of chiller system models focused on FDD Yan

  2020-08-04

  

  Another stream of chiller system models focused on FDD. Yan et al. (2018) used a back-tracing sequential forward feature selection algorithm to select the most significant features for FDD and then used the support vector machine for measuring accuracy. Li and Hu (2018) considered the density-based

• In this study we examined the role of a

  2020-08-04

  

  In this study we examined the role of a well characterized genetic polymorphism in the COMT gene in mediating cognitive antipsychotic treatment effects in first episode psychosis (FEP). We considered catechol-O-methyltransferase (COMT) to be a potentially important baseline consideration in a pharma

• Recent studies show that the expression and function

  2020-08-04

  

  Recent studies show that the expression and function of some ion channels such as voltage-gated potassium channels, sodium channels and calcium channels are closely related to the proliferation, migration, and invasion of tumor cells [40], [41], [42]. Firstly, the expression of ion channels is chang

• br Cocaine dependence is common

  2020-08-04

  

  Cocaine dependence is common, with over 1.5 million actively cocaine-dependent people in 2011 who have substantial social and economic morbidity from it, but it has no US Food and Drug Administration-approved pharmacotherapy (, ). In methadone maintenance programs rates of cocaine use range from 3

• RI-1 In summary the work by Park et al

  2020-08-04

  

  In summary, the work by Park et al. (2017) provides a strong evidence for the role of DNA damage in normal aging. By uncovering the link between activation of DNA damage and metabolic decline Park et al. (2017) demonstrate that the consequences of unrepaired DNA breaks go beyond mutations but also a

• Mexiletine HCl In this study using REMD with

  2020-08-04

  

  In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).

• Alternative splicing is a critical

  2020-08-03

  

  Alternative splicing is a critical part of regulating gene expression; over 90% of the human transcriptome is alternatively spliced [4]. Identifying the role of alternative splicing in the function of multiple biological and disease processes has driven many research initiatives in recent years [5].

• Neuroinflammation is the one of the

  2020-08-03

  

  Neuroinflammation is the one of the emerging causal factors contributing to these cognitive deficits. Therefore, we further tested the hypothesis that neuroinflammation is a key component contributing to the progression of spatial memory deficits during HH. Spatial memory deficits were observed afte

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