• Because of its excellent GPR

  2022-08-26

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, casr was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of 16

• Disrupting the dialog between microbiota and the host

  2022-08-26

  

  Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated

• With this goal in mind we proceeded to

  2022-08-26

  

  With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti

• d-glucose Based on work from our labs with mGlu

  2022-08-26

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

• The aim of our study was to investigate

  2022-08-26

  

  The aim of our study was to investigate the polymorphisms of RAGE and glyoxalase I gene and sRAGE serum levels in patients with pathological pregnancy trying to describe the genetic background of pathological pregnancy or to find a new biochemical marker (sRAGE) of these pathological states in pregn

• 77 br Brief overview of the glutamate system and

  2022-08-26

  

  Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric 77 (GABA), the primary inhibitory neurotransmitter. Together, GABA and

• In conclusion we have designed and characterized a novel ser

  2022-08-26

  

  In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,

• Genetic disruption or pharmacologic inhibition

  2022-08-25

  

  Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co

• br Conflicts of interests br Acknowledgements We

  2022-08-25

  

  Conflicts of interests Acknowledgements We thank Drs. T. Tomita and T. Iwatsubo (Tokyo University, Tokyo, Japan) for anti-presenilin 1-CTF antiserum, Dr. A. Takashima (Gakushuin University, Tokyo, Japan) for anti-Pen-2 antiserum and the laboratory members for helpful comments and discussion. M

• The synthesis of compounds and

  2022-08-25

  

  The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanediamin

• The overall very satisfactory potency profile of

  2022-08-25

  

  The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic EPZ004777 core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sens

• br FGF FGFR pathway as predictive

  2022-08-25

  

  FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m

• Results of studies on fish FBPase

  2022-08-25

  

  Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv

• Based on the inhibitory potency of

  2022-08-24

  

  Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o

• Two typical properties of Gi o protein coupled

  2022-08-24

  

  Two typical properties of Gi/o protein-coupled receptors, namely an increase in 35S-GTPγS binding (Strange, 2010) and an inhibition of exocytotic noradrenaline release (Schlicker and Göthert, 1998), were not shared by H4 receptor activation on cortical membranes (guinea-pig and mouse) and cortical s

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