• HET0016 Kinases belonging to the Thousand and one Tao family

  2022-02-24

  

  Kinases belonging to the Thousand and one (Tao) family are conserved throughout evolution. Three Tao proteins are encoded in the human genome (TAO1, TAO2, and TAO3), while D. melanogaster possesses a single ancestral Tao kinase (Tao-1). Like Hpo and GckIII, Tao kinases belong to the Sterile 20-like

• Almost all of the series and compounds

  2022-02-24

  

  Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri

• Introduction Epigenetic mechanisms modulate heritable phenot

  2022-02-24

  

  Introduction Epigenetic mechanisms modulate heritable phenotypic changes that are not dictated by changes in DNA sequences. The link between epigenetic modifications and cancer development has been established [1], [2]. Histone modifications represent an important class of epigenetic mechanisms tha

• The role of the cyclic AMP regulated exchange

  2022-02-24

  

  The role of the cyclic AMP regulated exchange factor Epac1 is emerging in cancer (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). Interestingly, in cancer cell migration, activation of Epac1 can be linked to activation of Rac. As s

• Another important question is what ligand s

  2022-02-24

  

  Another important question is what ligand(s) bind to GPR84 in vivo? Previous studies have identified medium-chain FFAs of 9 to 14 carbons in length and two other organic molecules (6-n-octylaminouracil and 3,3′-diindolylmethane) as agonists of GPR84 in vitro (Wang et al., 2006, Suzuki et al., 2013).

• The physiological and pharmacological roles

  2022-02-24

  

  The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po

• Compounds and were tested for pharmacodynamic effects in

  2022-02-24

  

  Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion at bo

• br Introduction The generic antifibrinolytic drug

  2022-02-23

  

  Introduction The generic antifibrinolytic drug tranexamic GSK J4 free base mg (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19]. Howev

• Moreover to evaluate the properties of

  2022-02-23

  

  Moreover, to evaluate the properties of immobilized β-glucosidase further, the anti-protease test was also carried out. The result showed that the residual activity of the β-glucosidase@ZIF-8 was higher than that of the nano-SiO2@β-glucosidase and free β-glucosidase. Because free β-glucosidase and t

• FFAs concentration response curves for increasing intracellu

  2022-02-23

  

  FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto

• The pharmacokinetic properties of were amenable to oral dosi

  2022-02-23

  

  The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ

• In a recent study Neelaveni

  2022-02-23

  

  In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported

• br Acknowledgments We apologize to the researchers who

  2022-02-23

  

  Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R0

• More recently the JmjC domain histone

  2022-02-23

  

  More recently, the JmjC domain histone H3K36 di-demethylase KDM2B/FBXL10 has also been shown to play an important role in definitive hematopoiesis [17]. Kdm2b is highly expressed in the HE, and its deletion (Tie2) caused embryonic lethality due to a precipitous drop in the number of hemogenic endoth

• Several named antagonist ligands have figured noticeably in

  2022-02-23

  

  Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l

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