• Strengths The primary feature of GPR agonists resides

  2022-04-11

  

  Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L cholecystokinin receptor as well as glucose-dependent insulin secretion and insulin promoter activity enhanc

• While NR upregulation in the spinal cord is known

  2022-04-11

  

  While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1

• Capillary monolithic columns obtained by in situ

  2022-04-11

  

  Capillary monolithic columns obtained by in situ polymerization have been developed rapidly as an efficient chromatographic stationary phase, which exhibits excellent reproducibility, reliable stability and fast transfer kinetics [18]. Recently, it has been extensively applied in capillary liquid ch

• The amino hydroxy methyl isoxazolepropionic acid

  2022-04-11

  

  The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic KL 001 (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1, GluA3, or GluA4 subu

• Several studies have shown that regulation

  2022-04-11

  

  Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu

• MAPK are involved in a large variety

  2022-04-09

  

  MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER

• br Acknowledgements br Introduction Ghrelin is a potent orex

  2022-04-09

  

  Acknowledgements Introduction Ghrelin is a potent orexigenic hormone and growth hormone secretagogue mainly derived from the stomach [1], [2], [3], [4], [5]. Other pleiotropic actions of the hormone include those that are glucoregulatory, food reward-enhancing, gastric motility-enhancing, and

• It was recently reported that aged GHSR mice in

  2022-04-09

  

  It was recently reported that aged GHSR−/− mice, in addition to showing alterations in meal pattern microstructure, exhibit NPY and AgRP mRNA upregulation in the ARC [56]. After an overnight fast, our animals exhibited a similar pattern of upregulated NPY and AgRP mRNA expression. Given that GHSR1a

• Optimization of the tetrahydroindazole series

  2022-04-09

  

  Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ().

• br Introduction Alzheimer s disease AD

  2022-04-09

  

  Introduction Alzheimer's disease (AD) affects ca. 46 million people worldwide [1] and it is expected that the number will double or triple by 2030 or 2050, respectively, while no significant progress has been made in research for early diagnosis and new efficient therapies. Currently available me

• Methoxyflavone and methoxyflavanone Fig both

  2022-04-09

  

  6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl

• In summary the SAR of a series of

  2022-04-09

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty Rhapontigenin receptor receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded

• Over decades a deeper understanding of terpene

  2022-04-09

  

  Over decades, a deeper understanding of terpene synthases has also permitted enzyme engineering for unnatural substrate acceptance. Novel terpenoids have been successfully synthesized from substrate analogues as by-products from mechanistic investigation (Faraldos et al., 2012; Miller, Yu, & Alleman

• hcv protease inhibitor Data are expressed as means

  2022-04-09

  

  Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of hcv protease inhibitor expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, i

• In patients with breast cancer ZRANB gene

  2022-04-09

  

  In patients with breast cancer, ZRANB1 gene amplification was found in a subset of cases, and ZRANB1 protein levels correlated with EZH2 protein levels and poor survival (both TNBC and non-TNBC). Moreover, unlike normal mammary epithelial cells, all human breast cancer cell lines examined (both TNBC

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