• To obviate the mitogenic FGF

  2021-10-27

  

  To obviate the mitogenic FGF19 activity, several engineered FGF19 variants have been generated aiming to maintain the metabolic activity excluding the protumorigenic ones. One variant, M70, that differs from wild-type FGF19 by 5-amino acids deletion at the N-terminus and the substitution of 3-amino

• Binding of FGFs to FGFRs leads

  2021-10-27

  

  Binding of FGFs to FGFRs leads to receptor dimerization, resulting in the transphosphorylation of a tyrosine in the activation loop of the kinase domain. Subsequently, the activated FGFRs phosphorylate their intracellular receptor substrates, particularly FGFR substrate 2 (FRS2) and phospholipase Cγ

• Defining the cooperation between molecular pathways

  2021-10-27

  

  Defining the cooperation between molecular pathways within highly complex biological systems, such as those between immune cell networks and target tissues is certainly a hard task. Recently, there are many investigations in the pathogenesis of renal graft rejection, one of the most evident investig

• Sirolimus rapamycin and everolimus both of

  2021-10-27

  

  Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that pr

• Last we demonstrate that the role of

  2021-10-27

  

  Last, we demonstrate that the role of EZH2 as a transcriptional activator, with AR being a key target, coexists with its conventional catalytic role in gene repression and plays important oncogenic functions in AR-driven PCa (Figure 7F). Enzymatic EZH2 inhibitors such as EPZ and GSK126, although eff

• br Conflict of interest br Author contributions br Introduct

  2021-10-27

  

  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

• br Conclusion and future perspectives In the setting of myoc

  2021-10-26

  

  Conclusion and future perspectives In the setting of myocardial I/R stress, HDAC activity is induced and contributes to myocardial injury. HDAC inhibition appears to protect the PYR-41 from I/R injury by activating a variety of pro-survival molecular pathways. From a clinical relevance standpoin

• Screening of the compounds allowed for

  2021-10-26

  

  Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr

• br Conclusion br Introduction The intracellularly generated

  2021-10-26

  

  Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri

• Recently a lot of synthetic FFA agonists containing acidic

  2021-10-25

  

  Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2

• According to Laplace s law loss of myogenic response

  2021-10-25

  

  According to Laplace’s law, loss of myogenic response would increase wall stress and tension in downstream vessels and subsequently induce endothelial dysfunction and arterial stiffness [36]. Indeed, we found that arteries from FPR-1 KO mice presented with a leftward shift in the stress-strain curve

• Consistently with the above discoveries it

  2021-10-25

  

  Consistently with the above discoveries, it has been also shown that in cardiomyocytes with shRNA-down-regulated FBP2, mitochondria are more susceptible to depolarisation (Gizak et al., 2012a) and H2O2-induced oxidative stress (Wiśniewski et al., 2017). In OG-L002 overexpressing FBP2 (cardiomyocyte

• Acetylation of histones by histone acetyltransferases stimul

  2021-10-25

  

  Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Nogo-66 (1-40) structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recent stu

• To date several studies have suggested that serum HER

  2021-10-25

  

  To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i

• Importantly recent in vivo results demonstrated that combini

  2021-10-25

  

  Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla

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