• Nuclear export of GK has been reported to be dependent

  2022-06-23

  

  Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros

• br Discussion According to the generally accepted notion whi

  2022-06-22

  

  Discussion According to the generally accepted notion which originated from the study of ATP-depleted NAD/NADH Quantitation Colorimetric Kit the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and t

• LXRs are physiological regulators of cholesterol and

  2022-06-22

  

  LXRs are physiological regulators of cholesterol and lipid metabolism and influence glucose metabolism. In addition, they have been shown to repress transcription of certain pro-inflammatory genes (Jakobsson et al., 2012; Ogawa et al., 2005; Terasaka et al., 2005). Thus, LXRs can either activate or

• GLP is released in response to ingestion

  2022-06-22

  

  GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty sodium butyrate receptor 4 (FFA4/GPR120) as a potential 7TM receptor involv

• In addition to the four classical FGFRs

  2022-06-22

  

  In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i

• The precise mechanism by which erastin inhibits

  2022-06-22

  

  The precise mechanism by which erastin inhibits SLC7A11-mediated cystine import it still unknown. The initially proposed mechanism, by which erastin binds a related transport protein, SLC7A5, and inhibits SLC7A11 in trans [25], was revised soon after, and it was suggested that erastin inhibits SLC7A

• Introduction High mobility group box HMGB

  2022-06-22

  

  Introduction High mobility group box 1 (HMGB1) is a nuclear protein that plays a fundamental role in the regulation of DNA-associated events such as DNA repair, transcription, and replication. HMGB1 can be translocated to the cytosol, plasma membrane, and extracellular space in response to various

• Fas ligand FasL the natural ligand of Fas

  2022-06-22

  

  Fas ligand (FasL), the natural ligand of Fas, can interact with Fas and thus induce cell apoptosis through the cascade of death signal in various cell types [8]. Additionally, Fas, which is a member of the tumor necrosis factor (TNF) receptor superfamily and death receptor family, is one kind of tra

• Compounds and were evaluated for their pharmacokinetic prope

  2022-06-22

  

  Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure

• br Conflict of interest br

  2022-06-22

  

  Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu

• Histamine which was used as the agonist had low potencies

  2022-06-22

  

  Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct

• YAP TAZ nuclear function is also influenced by

  2022-06-22

  

  YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 lgk974 exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ binding to T

• br Conflict of interest statement br Introduction The

  2022-06-22

  

  Conflict of interest statement Introduction The Hedgehog (Hh) family of secreted protein signals patterns many tissues and structures during embryogenesis (Chiang et al., 1996, Dessaud et al., 2008, Ingham, 1993) and, post-embryonically, governs tissue homeostasis and regeneration by regulatin

• KYNA has been shown to regulate iNKT

  2022-06-21

  

  KYNA has been shown to regulate iNKT cytokine release (Fallarini et al., 2010) and at high concentrations to reduce LPS-induced TNFα release from cultured peripheral blood mononuclear line (Wang et al., 2006). Our results show that elevating KYNA to “exercised” levels is sufficient to promote an ant

• In summary through medicinal chemistry design

  2022-06-21

  

  In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d

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