• In the present study we investigated

  2022-10-08

  

  In the present study, we investigated the mechanisms underlying the ability of 5-FU to modify histone acetylation. Our results suggested that 5-FU induces global histone de-acetylation in CRC by promoting the degradation of p300 and CBP, two important homologous HATs catalyzing acetylation at multip

• The presence of the H receptor in

  2022-10-08

  

  The presence of the H3 receptor in humans was confirmed approximately 25 years ago, and the receptor was successfully cloned in 1999 (Thurmond, 2010). The H3 receptor is unique, as it controls feedback of histamine release, particularly in the central nervous system, where it modulates neurotransmit

• The beta catenin TCF complex is an important

  2022-10-04

  

  The beta-catenin/TCF complex is an important target in the Wnt/beta-catenin pathway. This complex has proven challenging to target. However, natural inhibitors of this complex have been identified. One group of inhibitors is called the inhibitors of Wnt response (IWR-1/2). IWR-1/2 targets Axin and s

• br Materials and methods br Results br

  2022-10-04

  

  Materials and methods Results Discussion Although there is general agreement that GPR109A has anti-lipolytic activity and that the NEFA reduction in response to nicotinic inhibitor of catalase is mediated by GPR109A, whether GPR109A activation has any impact on plasma TG levels is unclear.

• GPR has been implicated in neuropathic and inflammatory pain

  2022-10-04

  

  GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow

• br Author contributions br Acknowledgements The

  2022-10-04

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• For another the N terminal sequence of

  2022-10-03

  

  For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal

• Glucagon was described as an insulin secretagogue as early

  2022-10-03

  

  Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β porcn clearly show that glucagon is capa

• br Methods br Results br

  2022-10-03

  

  Methods Results Discussion Previous work by the Hirano group investigated the effect of GIP in murine atherosclerotic models and found infusion of GIP (1–42) by osmotic mini-pumps to decrease lesion size after 4 weeks in non-diabetic as well as in diabetic ApoE−/− mice [8], [9]. Mechanistic

• Our initial lead optimization started with the modification

  2022-10-03

  

  Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li

• The cortical actin filaments are

  2022-10-02

  

  The cortical TCS JNK 6o filaments are arranged in a network abuting the plasma membrane with a thickness of ∼190nm in living cells, that displays highly dynamic behaviors 15, 16, 17. Technical challenges, however, have hampered investigation of the detailed function dynamic interactions between the

• In C elegans KDM A appears

  2022-10-02

  

  In C. elegans, KDM4A appears to be involved in H3K36me3 reduction on the X chromosome, suggesting that this protein has a relevant role in germ cell development (Figure 2A) (47). In addition, in HeLa cells, KDM4A is associated with the repression of the achaete-scute complex homologue 2 (ASCL2) gene

• We observed that the Toc G domain

  2022-10-01

  

  We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate

• br GSK Glycogen synthase kinase GSK is a ubiquitous

  2022-10-01

  

  GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d

• Recently we suggested that KYNA an endogenous GPR agonist co

  2022-10-01

  

  Recently, we suggested that KYNA – an endogenous GPR35 agonist could be produced in a human cornea since we showed the presence of the enzymes that catalyze the synthesis of KYNA – kynurenine aminotransferases I-III in corneal epithelium, stroma and endothelium (). Therefore, these findings provided

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