• An alternative approach to improving pharmacokinetic profile

  2021-12-02

  

  An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl

• br Introduction HH GLI signaling is one of

  2021-12-02

  

  Introduction HH-GLI signaling is one of the major pathways involved in both normal and neoplastic development [[1], [2], [3], [4]]. Inappropriate activation of this pathway has been linked to cancer, including medulloblastoma, rhabdomyosarcoma, basal cell carcinoma and cancers of the lung, stomac

• The overall very satisfactory potency

  2021-12-02

  

  The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Temsirolimus receptor core in order to improve affinity to FFA1. The agonist activity in this series appears to be part

• AZ191 Potential roles for S P in angiogenesis cancer and

  2021-12-02

  

  Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-

• br Place in Therapy In the case of minor

  2021-12-02

  

  Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito

• We have expanded these studies by doing

  2021-12-02

  

  We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA Zanamivir mg or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagon

• The beta catenin TCF complex is an important

  2021-12-02

  

  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 Ketone body metabolism and neuronal excitability One of t

  2021-12-02

  

  Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona

• To apply the recently developed GPR ligands

  2021-12-02

  

  To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the Conoidin A and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the

• In order to discover novel small molecule compounds

  2021-12-01

  

  In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev

• Recently several dual GLP GIP receptor agonists have been

  2021-12-01

  

  Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously

• Although the ramifications of non additive

  2021-12-01

  

  Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no

• Another lever to efficiently eradicate tumors including ovar

  2021-12-01

  

  Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing

• Although angiogenesis is crucial for

  2021-12-01

  

  Although angiogenesis is crucial for cerebral ischemic rehabilitation, the mechanism underlying NGF promotion of angiogenesis is not clear. Previous studies showed that angiogenesis can be promoted by FAK, in a breast cancer model [19]. Recent studies showed that FAK phosphorylation participated in

• Ramelteon The progression of HIV varies from patient to pati

  2021-12-01

  

  The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these

15395 records 505/1027 page Previous Next First page 上5页 501502503504505 下5页 Last page