• Given the potency enhancing effect of the butyl

  2021-07-03

  

  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 action of pt PGE

  2021-07-03

  

  The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in

• br Enzyme activations Activated proteinases can unleash a

  2021-07-03

  

  Enzyme activations Activated proteinases can unleash a deluge of tissue damage (Zucker et al., 2009). Once activated, the essential enzymes such as serine proteases and cysteine proteases cannot discriminate between self and non-self, burning away self-tissues (Chien et al., 2009, Laskar et al.,

• The synthetic routes to the substrates based on

  2021-07-03

  

  The synthetic routes to the substrates based on the 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene cores are depicted in Scheme 3. A Michael-type glycosylation of 2,3-dihydroxynaphthalene 16a gave the acetylated sugar 17a which was deprotected giving the required β-glucosidase sub

• In the previous study glutamyl endopeptidase of B intermediu

  2021-07-03

  

  In the previous study glutamyl endopeptidase of B. intermedius has been reported to be distributed in the Immunology Inflammation Compound Library of B. intermedius as follows: 90% of synthesized enzyme has been detected in the culture liquid, 9.3% of glutamyl endopeptidase—in the fraction of membr

• According to the Nomenclature Committee of the International

  2021-07-03

  

  According to the Nomenclature Committee of the International Union of Biochemistry and Molecular Biology (NC-IUBMB, 1992), peptidases are divided into two classes, namely exopeptidases and endopeptidases, based on their actions on substrates and their active sites, respectively. Endopeptidases inclu

• As retinol was not inducing any of the isoforms of

  2021-07-03

  

  As retinol was not inducing any of the isoforms of CYP450 responsible for the bioactivation of paracetamol, we decided to examine retinol's effect on renal and hepatic glutathione to determine whether retinol was potentiating hepatotoxicity through a mechanism of glutathione depletion. Studies, util

• The molecular mechanisms regulating the differentiation of

  2021-07-03

  

  The molecular mechanisms regulating the differentiation of Th1 versus Tfh Chlorhexidine digluconate from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cel

• Modulating protein stability specifically inhibiting ubiquit

  2021-07-03

  

  Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here

• Moving forward the new mathematical model opens

  2021-07-03

  

  Moving forward, the new mathematical model opens doors for understanding the SCF network, where activity of a component is blunted through mutation or altered in expression in diseased states, and during therapeutic intervention. Computational modeling could reveal underappreciated secondary or tert

• DNA methylation assay To test the biological activity of pur

  2021-07-02

  

  DNA methylation assay. To test the biological activity of purified A1S_0222, a methylation assay was performed using the Int1 DNA. As an alternative DNA substrate, Seq3 (located in gene A1S_0965 of A. baumannii ATCC 17978) was amplified from Acinetobacter baumannii 29D2 using the oligonucleotides Se

• Deregulated Wnt signaling either due to pathway mutations

  2021-07-02

  

  Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen

• MTT results show that both pancreatic cell lines were

  2021-07-02

  

  MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)

• Besides the assessment of toxicological effects immediately

  2021-07-02

  

  Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c

• It remains unclear how LINE RNA Nucleolin

  2021-07-02

  

  It remains unclear how LINE1 RNA-Nucleolin-Kap1 are targeted to the Dux cluster. LINE1-Nucleolin-Kap1 may have other interacting partners with DNA binding specificity. For example, YY1 has been implicated in targeting a repressive complex containing Nucleolin to the human DUX4 cluster (Gabellini et 

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