• Metal ions are known not to be

  2020-06-20

  

  Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe

• br Rationale and hypothesis To discover an allosteric inhibi

  2020-06-20

  

  Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be

• Because of the important role of the DDB CUL

  2020-06-20

  

  Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup

• Of the acidic hydroxyazoles involved

  2020-06-20

  

  Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the

• Previous synthetic lethal screening efforts Cox et

  2020-06-20

  

  Previous synthetic lethal screening efforts (Cox et al., 2014) have mainly used RNAi as a means of identifying potential targets (Barbie et al., 2009, Kim et al., 2016, Luo et al., 2009, Scholl et al., 2009), although a few screens (Shaw et al., 2011, Steckel et al., 2012) have been performed with s

• Although PQQ has nutritional importance and pharmacological

  2020-06-20

  

  Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov

• Widely expressed mammalian adhesion receptors for fibrillar

  2020-06-20

  

  Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.

• In conclusion our data demonstrated that montelukast

  2020-06-20

  

  In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va

• br Conflicts of interest br Acknowledgments This research wa

  2020-06-19

  

  Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest

• The first transcription factor TF known to interact with

  2020-06-19

  

  The first transcription factor (TF) known to interact with one of the cis-acting GAREs is GAMYB protein, the expression of which is induced by GA in the aleurone Tenovin-1 receptor of barley (HvGAMYB) (Gubler and Jacobsen, 1992). GAMYB is an important regulator of endosperm functions during seed dev

• Acknowledgements This work was supported in

  2020-06-19

  

  Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou

• The enantiomeric ratio ER of chiral compounds

  2020-06-19

  

  The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o

• br Results br Discussion The

  2020-06-19

  

  Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i

• It was reported that the

  2020-06-19

  

  It was reported that the expressions of DPP-4 and SDF-1α increase through HIF-1α [27], [28]. Myocardial ischemia by MI enhanced the DPP-4 and SDF-1α levels in myocardium in the present study. SDF-1α is released from cardiomyocytes and has beneficial effects on cardiomyocytes through SDF-1α/CXCR4 aft

• We have reported previously that aminoacrylate

  2020-06-19

  

  We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD

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