• In respect of clinical development Takeda

  2022-02-11

  

  In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul

• The molecular identity of RA

  2022-02-11

  

  The molecular identity of RA’s target during LTP induction was determined by pharmacological testing. The inhibitory effects of CNQX and niflumic acid on LTP induction remained even in the presence of RA, indicating RA did not affect either the AMPA receptor nor chloride channel (Fig. 2B and D) [26]

• PKI-402 Nuclear export of GK has been reported to

  2022-02-11

  

  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

• GCK MODY is the most common

  2022-02-11

  

  GCK-MODY is the most common form of MODY diabetes in many populations (Chevre et al., 1998; Massa et al., 2001; Barrio et al., 2002; Estalella et al., 2007; Pruhova et al., 2010; Capuano et al., 2012; Giuffrida et al., 2017). However, data about GCK-MODY among North African populations are very rare

• Growing evidence supporting the anti inflammatory and tissue

  2022-02-10

  

  Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a

• The precise mechanism by which erastin

  2022-02-10

  

  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

• FBPase deficiency is a very rare

  2022-02-10

  

  FBPase deficiency is a very rare inborn error of fructose Zanamivir of autosomal recessive inheritance. This disorder usually occurs in the first year of life through ketotic hypoglycemia and lactic acidosis triggered by catabolic episodes such as prolonged fasting or febrile infections (Steinmann

• However T DM and associated hyperglycemia can adversely

  2022-02-10

  

  However, T1DM and associated hyperglycemia can adversely affect the structure and function of the heart in several mechanisms including inhibiting the anabolic effect of insulin due to its deficiency, generation of higher levels of ROS and induction of lipid peroxidation, and subsequent activation o

• Mitochondrial is the main source for ROS and ATP generation

  2022-02-10

  

  Mitochondrial is the main source for ROS and ATP generation, and the loss of mitochondrial membrane potential is involved in the alteration of mitochondrial metabolism and mitochondrial failure-induced cell death [33,34]. In this study, we showed that upregulated ZNF32 sustained mitochondrial membra

• Macrocycle was synthesized as described

  2022-02-10

  

  Macrocycle was synthesized as described in , . Under SAr conditions, 2-chloronicotinonitrile was heated with -butyl 5-aminopentanoate in refluxing ethanol (). The resulting aminopyridine was treated with mesyl chloride and the nitrile was subsequently reduced to afford amine . Chloroaminopyrimidin

• AIM-100 It has been shown that mice lacking SMAD in

  2022-02-10

  

  It has been shown that mice lacking SMAD2 in T cells do not develop spontaneous lymphoproliferative autoimmunity (Malhotra et al., 2010). Further, FOXO1 is known to activate proinflammatory MCP-1 and IL-6 (Ito et al., 2009). To this end, we also validated the downstream target FOXO1 and SMAD2 after

• br Sources of funding This work was supported by

  2022-02-10

  

  Sources of funding This work was supported by grants from the Canadian Institutes of Health Research (CIHR) (No. MOP-111096) and from the Heart and Stroke Foundation of Canada awarded to Dr. Danielle Jacques. Disclosures Acknowledgments Introduction A large number of epidemiological, hu

• 1670 Theoretically the majority of resistance mechanisms

  2022-02-10

  

  Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei

• filipin Since its development the HCV replicon system Lohman

  2022-02-10

  

  Since its development, the HCV replicon system (Lohmann et al., 1999) has been a critical tool in the HCV antiviral discovery process (Gottwein et al., 2009, Imhof and Simmonds, 2010, Lohmann et al., 1999, Pietschmann et al., 2001, Imhof and Simmonds, 2010, Gottwein et al., 2009). The replicon assa

• Salmeterol xinafoate synthesis br Structural studies of GCAP

  2022-02-10

  

  Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding Salmeterol xinafoate synthesis to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-termin

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