• Recently several Pt IV complexes

  2020-11-05

  

  Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with

• br Effects of estrogens on

  2020-11-05

  

  Effects of estrogens on bone Estrogens play an important role in bone remodeling, as demonstrated by studies in mice in which the ER genes were deleted [21], [22]. ERβ compensates for the A-1210477 synthesis of ERα, and vice versa, but when both ERs are deleted a profound decrease in trabecular b

• In summary we have identified a series

  2020-11-05

  

  In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als

• Previous studies demonstrated that cPLA translocates to the

  2020-11-05

  

  Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at

• br Materials and methods br

  2020-11-05

  

  Materials and methods Results Discussion We recently detected phosphorylation of tyrosine Y102 in BPV-1 E2 and reported that FGFR3 binds to E2 and limits E1 dependent viral DNA replication (Culleton et al., 2017, Xie et al., 2017). In the current study, we addressed the potential role of ot

• Besides being the only enzyme E

  2020-11-05

  

  Besides being the only enzyme, E1 is also the largest and arguably most complex protein encoded by papillomaviruses. As the replicative helicase, E1 plays a central role in the viral life cycle. To do so, E1 engages in multiple protein–protein and protein–nucleic L-α-Aminoadipic Acid interactions to

• br Ubiquitination and deubiquitination pathways Ubiquitinati

  2020-11-05

  

  Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec

• br Introduction Biocatalysis can be used to

  2020-11-05

  

  Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc

• In conclusion DDR ECD was shown to be

  2020-11-05

  

  In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E

• Finally the identification of predictive

  2020-11-05

  

  Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and

• Kim et al reported for bioactive compounds originating from

  2020-11-05

  

  Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b

• The H E staining and Nissl staining results showed that

  2020-11-05

  

  The H&E staining and Nissl staining results showed that damage to the pyramidal neurons in the CA1 and CA3 regions of the hippocampus were observed in the 50 mg/kg/day DBP group, accompanied by an absence of Nissl bodies, suggesting that DBP exposure can lead to pathological changes in the neurons o

• br Structure and function of EPAC isoforms EPACs are guanine

  2020-11-05

  

  Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr

• The TELI results of DNA

  2020-11-04

  

  The TELI results of DNA damage responses to CAA and SO then informed our choice of bacterial strains in subsequent experiments. We investigated E. coli cellular survival in response to CAA and SO exposure by determining the sensitivity of a number of E. coli strains, each possessing single or multip

• Acidic substituents showed moderate biochemical

  2020-11-04

  

  Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic XAP044 sale were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical

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