• Results of the present study demonstrate that OHC treatment

  2019-12-16

  

  Results of the present study demonstrate that 25-OHC treatment of THP-1 monocytes induced vimentin intermediate filament reorganization to more cortical structures and a polarized phenotype (Fig. 5). Vimentin is the major intermediate filament protein present in leukocytes and plays an important rol

• UBA belongs to the non canonical E

  2019-12-16

  

  UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5\'s adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral

• All DGKs have at least

  2019-12-16

  

  All DGKs have at least two cysteine-rich regions homologous to the C1A and C1B motifs of PKCs [26]. In theory, these domains may bind DAG, perhaps localizing DGKs to where DAG accumulates. However, no DGK C1 domain has so far been conclusively shown to bind DAG. In fact, structural predictions sugge

• br Materials and methods br Results Metabolic stability of

  2019-12-16

  

  Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only

• br Transparency document br Introduction The cyclic nucleoti

  2019-12-16

  

  Transparency document Introduction The cyclic nucleotide adenosine 3′,5′-cyclic monophosphate (cAMP) exerts both an endothelium-dependent and an endothelium independent vasorelaxant action in rat PD 151746 [1]. cAMP direct, endothelium-independent vasorelaxant effects have been attributed to s

• N Cyclopentylmethyl analog exhibited fold less potent recept

  2019-12-16

  

  N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl

• br When Does Activity with Alternative

  2019-12-16

  

  When Does Activity with Alternative Substrates Depend on Neutral Drift? In a final scenario, the alternative reaction catalyzed by an enzyme might have no significant (positive or negative) effects on the system fitness, and thus it would be invisible to natural selection and essentially subject

• br Materials and methods br Results

  2019-12-16

  

  Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro

• chemokine receptor In vitro studies in NSCLC cell lines

  2019-12-16

  

  In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC chemokine receptor with Growth inhibition (GI50) values ranging from 7 to 32

• Several main strategies for targeting E s

  2019-12-16

  

  Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f

• br Introduction br Structure of the Ku

  2019-12-16

  

  Introduction Structure of the Ku heterodimer associated to DNA The atomic structure of the Ku heterodimer, alone and bound to a small DNA fragment, was recently determined (Walker et al., 2001) and has significantly improved our understanding of DNA recognition by DNA-PK holoenzyme (Fig. 3). B

• Like compound substitution on compound contains amino and ca

  2019-12-16

  

  Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.

• 3ct receptor Given the excellent in vitro pharmacology profi

  2019-12-16

  

  Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic 3ct receptor functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1

• The X ray crystal structure

  2019-12-16

  

  The X-ray crystal structure of palbociclib bound to CDK6 without a Cycloheximide (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V complex.

• br Genotype phenotype correlations Genotype phenotype correl

  2019-12-16

  

  Genotype-phenotype correlations Genotype-phenotype correlations are limited. Compared with individuals with truncating variants, those with pathogenic missense variants in the adenosine triphosphate binding site had a milder disorder, some with ability to walk unaided, better hand use, and less r

16044 records 937/1070 page Previous Next First page 上5页 936937938939940 下5页 Last page