• br Brief overview of GSK inhibitors We will briefly

  2022-08-02

  

  Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, diab

• Recently we suggested that KYNA an

  2022-08-02

  

  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

• The activation of the ERK pathway may participate in

  2022-08-02

  

  The activation of the ERK pathway may participate in the sensitization of primary afferents in pain transmission (Ji et al., 2009, Lai et al., 2011); the blockade of ERK activation in the DRG can decrease mechanical and heat hypersensitivity in inflammatory pain. IL-10 can inhibit phosphorylation of

• Ristocetin A sulfate synthesis GnRH ant have been designed t

  2022-08-02

  

  GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p

• Experiments conducted on the human parasite Leishmania major

  2022-08-02

  

  Experiments conducted on the human parasite Leishmania major has shown that specific parasitic antigens are involved in steering the immune responses to “protective” as opposed to “disease” state (Reiner et al., 1993; Reiner and Locksley, 1995; and Sjölander et al., 1998) and that antigenic composit

• In glioma or glial derived primary brain tumors

  2022-08-02

  

  In glioma, or glial-derived primary HC-030031 tumors, as in other cancers, glutathione is an important survival mechanism. Glioma cells are dependent upon SXC-mediated cystine uptake for viability, as they require intracellular cystine/cysteine for GSH synthesis (Ogunrinu and Sontheimer, 2010, Sont

• To confirm the in vitro findings atorvastatin

  2022-08-02

  

  To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g

• br Regulation of GCK by

  2022-08-02

  

  Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin

• Introduction Glucose dependent insulinotropic polypeptide GI

  2022-08-02

  

  Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G

• Piezo channels can be activated by many

  2022-08-02

  

  Piezo channels can be activated by many mechanical stimuli . While some of these stimulations directly mimic physiological forces experienced by vasopressin receptor antagonist , such as shear stress applied in a microfluidic chamber, the most commonly used modes of stimulation consist of stretchi

• br Pannexins which form channels connecting cells

  2022-08-02

  

  Pannexins, which form channels connecting Kif15-IN-1 with the extracellular environment, have also been studied in the setting of NASH. When open these channels participate in inflammatory processes. A decrease in lobular inflammation and oxidative stress was observed in mice with pannexin deleti

• Formyl peptide receptors FPRs are a family of

  2022-08-02

  

  Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on

• As demonstrated by Bayliss Bayliss

  2022-08-02

  

  As demonstrated by Bayliss Bayliss, [22] myogenic response is the ability of the blood vessels to contract in response to intraluminal pressure elevation. This is intrinsic to VSMCs, particularly in small arteries (dimeter Losmapimod polymerization within VSMCs in response to increased intravascula

• Considering together the conformational docking and SAR resu

  2022-08-02

  

  Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req

• To date increasing evidence has

  2022-08-02

  

  To date, increasing evidence has demonstrated that dysregulated lncRNAs are closely associated with the tumorigenesis and development of HCC via ceRNA modes [29,30]. LncRNAs could bind with special miRNAs and abrogate the inhibitory effect of these miRNAs on their targeted transcripts. For example,

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