• Toxicity is the main reason

  2025-01-04

  

  Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele

• br In our experience br History of ER and ACh

  2025-01-04

  

  In our experience History of ER and ACh tests As shown in Table 1, Stein et al. first reported the usefulness of intravenous injection of ER in diagnosing coronary insufficiency in 1949 [16]. In 1972, the first ER spasm provocation test was employed at the Cleveland Clinic during cardiac cathe

• We have previously shown that the antinociceptive effect of

  2025-01-04

  

  We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific Loxapine Succinate blockade or activation (Rojas-Corrales et al., 2000). Mo

• At present drugs that specifically inhibit YAP activity are

  2025-01-04

  

  At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi

• br Autophagy inducers Macroautophagy is often seen as a cell

  2025-01-04

  

  Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of Z-Ligustilide and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sensitivity

• To test the compounds metabolic stability

  2025-01-04

  

  To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura

• Recent studies have indicated that

  2025-01-04

  

  Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ aristocort australia have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pah

• Our results clearly demonstrate that inhibition of ATM pathw

  2025-01-04

  

  Our results clearly demonstrate that inhibition of ATM pathway activation results in resistance to Vγ2Vδ2 T cell-mediated cell death. Therefore, enhancing ATM activation along with Vγ2Vδ2 T cell treatment would promote the cytotoxicity of resistant ovarian cancer cells. To our knowledge, this is the

• br Introduction In the past two decades graphene

  2025-01-04

  

  Introduction In the past two decades, graphene and graphene based nanomaterials with unique physicochemical properties have attracted great attentions in many fields including biomedicine and biotechnology. Graphene oxide (GO) and its derivatives have shown promising potential as biological and c

• In previous years evidence emerged that inferred

  2025-01-04

  

  In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic LDN193189 BMP signaling (7) and piceatannol (8) (Fig. 3b) on mammalian arginase

• The crucial role of AP in establishing and maintaining cell

  2025-01-04

  

  The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch

• Anti-inflammatory agent br HMG proteins mobile modulators of

  2025-01-04

  

  HMG proteins: mobile modulators of chromatin structure and cellular phenotype The term “High Mobility Group” was originally coined for the HMG proteins because of their unusual solubility properties, their small size and their rapid mobility, relative to other chromatin proteins, during gel elect

• Plant defensins Vriens et al and linear

  2025-01-04

  

  Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et 

• br Introduction AMPA receptors AMPARs mediate the majority o

  2025-01-03

  

  Introduction AMPA receptors (AMPARs) mediate the majority of fast excitatory postsynaptic currents (EPSCs) in the 3mb (Jonas, 2000). The brevity of EPSCs and rapid deactivation of AMPARs depend upon a short lifetime of synaptically released glutamate, estimated to be about 1 ms (Clements et al.,

• Further validation for a role in LOX pathway

  2025-01-03

  

  Further validation for a role in 12/15-LOX pathway in mediating adipocyte function comes from studies revealing a regulatory role of lipocalin-2 on 12/15-LOX activity. Lipocalin-2, a glycoprotein member of the lipocalin superfamily, is a novel abundant adipokine implicated in obesity-mediated inflam

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