• Introduction Cytochrome P CYP A

  2020-03-23

  

  Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The Cy7 NHS ester (non-sulfonated) level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug respo

• Even minor alterations in the surfactants structure could ha

  2020-03-21

  

  Even minor alterations in the surfactants structure could have consequences on their physico-chemical characteristics; mono-RLs have less solubility, stronger surfaces sorb, and stronger cationic metals binding than homologue di-RLs (Zhang et al., 1997). The HPLC separation of RLs structure is base

• Estrogen receptor related receptor ERR like other members

  2020-03-21

  

  Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc

• Based on the similar activities of Rad p and

  2020-03-21

  

  Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC

• Most enzymes involved in the addition and removal of ubiquit

  2020-03-21

  

  Most prostaglandin receptor involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 l

• A great deal of research has focused on candidate

  2020-03-21

  

  A great deal of research has focused on candidate medications to modulate dopaminergic mechanisms through which psychomotor stimulants produce addictive effects, i.e., drugs that expressly target the DA transporter, D1-like receptor, or D2-like receptors., , However, effective dopaminergic-based ph

• An even more striking difference is

  2020-03-21

  

  An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97

• To overcome problems with the biochemical reconstitution of

  2020-03-21

  

  To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a

• Epothilone B Given the potency enhancing effect of the butyl

  2020-03-20

  

  Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti

• The larger eukaryotic ligases such as LigI and LigIV also

  2020-03-20

  

  The larger eukaryotic ligases, such as LigI and LigIV, also possess an additional N-terminal DNA-binding domain (DBD) that is required for efficient ligation (Fig. 1c) and enables these ligases to encircle DNA [17]. An equivalent helix–hairpin–helix domain is also present in the bacterial NAD-depend

• Our recent discovery M P H R A S of

  2020-03-20

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

• AMPK is a master regulator of metabolic homeostasis

  2020-03-20

  

  AMPK is a master regulator of metabolic homeostasis, its broad spectrum of metabolic activities makes it an attractive target for treatment of metabolic and related disorders including Diabetes and Obesity (Madhavi et al., 2018). It controls lipid metabolism through its target genes PPAR-γ, C/EBP-α

• Multiple lines of evidence now indicate that

  2020-03-20

  

  Multiple lines of evidence now indicate that mitochondrial decay is a fundamental factor that leads to alterations in energy metabolism in the aged heart (Hagen et al., 2002, Judge and Leeuwenburgh, 2007, Lesnefsky et al., 2001c). Nevertheless, the exact biochemical events that cause such an alterat

• Third we also found negative correlations between TREM mRNA

  2020-03-20

  

  Third, we also found negative correlations between TREM2 mRNA expression and the methylation rate of 4 CpG sites in the intron 1 of TREM2. Gene methylation rates are generally associated with gene expression. Thus, heavily methylated areas of genes are usually less active at the transcriptional lev

• br Experimental protocols br Acknowledgements This research

  2020-03-20

  

  Experimental protocols Acknowledgements This research was funded by the Croatian Ministry of Science, Education and Sports (Programmes 098-0982915-2948 and 098-0982522-2525), the Austrian Science Fund FWF (DK-MCD W1226, SFB LIPOTOX F30, P22832), and the Croatian-Austrian Intergovernmental S&T

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