• It has been reported that leukotrienes and

  2023-12-14

  

  It has been reported that leukotrienes and their receptors, e.g. the cysteinyl leukotriene receptor 1 (CysLT1) may promote closantel synthesis injury (Ding et al., 2007) and that increased 5-LOX expression and activity lead to production of brain-toxic molecules (Khan et al., 2010). However, differe

• Five alternatively spliced isoforms of ATX have been

  2023-12-14

  

  Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize

• Based on its kinetic parameters and quaternary structure R

  2023-12-13

  

  Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.

• Several strategies have been employed to

  2023-12-13

  

  Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, CMX001 induces changes in the spectral properties of the fluorophore(s) incorporated into t

• Furthermore a recently published network meta analysis inclu

  2023-12-13

  

  Furthermore, a recently published network meta-analysis including 30 trials in patients with hypertension and diabetes demonstrated that ARBs have efficacy similar to that of ACEIs for all-cause and cardiovascular mortality (HR 0.95, 95% CI 0.73 to 1.30 and HR 1.23, 95% CI 0.64 to 2.78, respectively

• br AR signals and chemosensitivity in

  2023-12-13

  

  AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance

• br Conclusions Our study confirms that N terminal mutations

  2023-12-13

  

  Conclusions Our study confirms that N-terminal mutations can affect Aβ fibril and oligomer formation, despite lying outside the core amyloid region of Aβ. Of the three factors that may influence Aβ-mediated toxicity (primary structure of Aβ, assembly structure and cellular responses), our results

• It thus appeared reasonable that AR needed

  2023-12-13

  

  It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]

• AdK as an important upstream regulator of adenosine based ho

  2023-12-13

  

  AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inh

• Despite these efforts to prevent oxidative

  2023-12-13

  

  Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of

• Despite functional studies demonstrating the role of HT in

  2023-12-12

  

  Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,

• The identification of novel kinase inhibitor scaffolds is

  2023-12-12

  

  The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y

• Two major categories of arginase inhibitors have been

  2023-12-12

  

  Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt

• Enhancers are short regions of DNA that

  2023-12-12

  

  Enhancers are short regions of DNA that are bound by DNA-binding proteins (TFs) to increase the likelihood of a particular gene to be expressed. Importantly, enhancers can be identified, and classified, by their patterns of chromatin accessibility and of enrichment in certain histone modifications.

• Various antiangiogenic drugs have been analyzed

  2023-12-12

  

  Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st

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