• Upstream Stimulatory Factor USF binding to the E

  2021-04-13

  

  Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran

• While the mechanism of DHODH inhibition induced differentiat

  2021-04-13

  

  While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,

• The folate pathway plays an essential role in cell

  2021-04-13

  

  The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec

• Acanthopanax senticosus Rupr Maxim Harms a

  2021-04-13

  

  Acanthopanax senticosus (Rupr. & Maxim.) Harms, a nontoxic herb belongs to the family of Araliaceae, which found in Northeast Asia. A. senticosus traditionally used as a tonic to treat rheumatism, diabetes, and hepatitis [7]. Previous phytochemical and biological investigations found its roots and s

• TNF a major cytokine that is critical in acute

  2021-04-13

  

  TNF-α, a major cytokine that is critical in acute and chronic inflammation, is responsible from chemotaxis, acute phase reactions and endothelial activation (Mahalingam and Karupiah, 1999). Our study showed that TNF-α is increased significantly in the pyelonephritic rats and montelukast displayed an

• In the course of our program which was aimed at

  2021-04-13

  

  In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys

• Unlike CRM exportins Cse and

  2021-04-13

  

  Unlike CRM1, exportins Cse1 and Xpot lack a C-extension and instead rely primarily on changes in HEAT-repeat conformation and direct Ran-cargo contacts to ensure low cargo-binding affinity in the cytosol and cooperative assembly of the exportin/Ran/cargo complex in the nucleus (Cook et al., 2005, Co

• Behaviors were compared between saline and amphetamine

  2021-04-13

  

  Behaviors were compared between saline and amphetamine pre-treatment groups at 24h and 2 weeks following the last treatment, or between pre-treatment groups that received vehicle or ASV-30 infusions, using separate two-way ANOVAs. Significant effects were analyzed further using Student–Newman–Keuls

• To investigate the mechanism of action of trisubstituted azo

  2021-04-13

  

  To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due

• Cisplatin br Results and discussion The results and subgroup

  2021-04-13

  

  Results and discussion The results and subgroup analysis of cholesterol and NCS from the both surveys are listed in Table 2 and shown in Fig. 1, A1 to E2. Common discussion Unlikely to the other NCS assays, a target value for cholesterol could be reported in the present survey. For NCS assays

• in the world In the horse oviduct the EP

  2021-04-12

  

  In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial in the world particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects differen

• TRAF and TRAF were initially identified as tumor

  2021-04-12

  

  TRAF1 and TRAF2 were initially identified as tumor necrosis factor receptor 2 (TNRF2)-associated components, TRAF4 was overexpressed in breast carcinoma cells, whereas TRAF3, TRAF5 and TRAF6 were discovered by their interaction with specific domains in the cytoplasmic tails of trans-membrane recepto

• br A brief introduction to DUBs The reversal

  2021-04-12

  

  A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating tryptophan hydroxylase (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be cl

• The activity of chromenones bearing heteroaryl

  2021-04-12

  

  The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue

• In light of the overall loss of activity

  2021-04-12

  

  In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The

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