• The number of small molecule GSK inhibitors is continuously

  2022-05-21

  

  The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop

• Because of its excellent GPR

  2022-05-21

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, N1-Methylpseudo-UTP 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

• Acknowledgments This research was supported by

  2022-05-21

  

  Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor

• gaba b br Clinical development of anti NASH drug therapies

  2022-05-21

  

  Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie

• Transporters are important ta http www

  2022-05-21

  

  Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea

• In the present study co administration of TM AT receptor

  2022-05-21

  

  In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury

• br Materials and methods br Results br

  2022-05-21

  

  Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen

• These findings raise the question of what mechanism

  2022-05-21

  

  These findings raise the question of what mechanism of beta cell proliferation is induced by short-term HF diet feeding. Gene expression profiling of isolated islets from mice fed a HF diet for 1 week revealed that expression levels of downstream genes of Foxm1 were coordinately upregulated (Fig. 5)

• br Materials and methods br Results br Discussion Our

  2022-05-21

  

  Materials and methods Results Discussion Our liver-specific Gck (−/−) mice and another line of liver-specific mice [13] exhibited impaired glucose tolerance. Furthermore, both knockout mice showed decreased hepatic glycogen content and reduced Pklr and Fas gene mi2 mg in the liver [11]. Ho

• Besides its established insulinotropic actions GIP has

  2022-05-21

  

  Besides its established insulinotropic actions, GIP has been shown to possess other direct beneficial effects on the beta cell, including stimulation of growth, differentiation, proliferation and survival.21, 22, 23 It has also been shown to stimulate proinsulin gene transcription and translation. M

• According to the aforementioned preclinical and clinical

  2022-05-21

  

  According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu

• Tail group SAR of the imidazole derived analogs is shown

  2022-05-21

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl

• Several observations about structure activity relationships

  2022-05-20

  

  Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic 2-Amino-ATP class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage

• Our results further indicate that low expression of

  2022-05-20

  

  Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi

• We have previously reported on the

  2022-05-20

  

  We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t

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