• br Materials and methods br

  2020-12-11

  

  Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s

• Anidulafungin br Materials and methods br Results br Discuss

  2020-12-11

  

  Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi

• An ideal CHK inhibitor would be minimally cytotoxic

  2020-12-11

  

  An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th

• In summary A is a potent

  2020-12-11

  

  In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste

• A French cohort study reported that micronized progesterone

  2020-12-11

  

  A French cohort study reported that micronized progesterone or didrogesterone used with oral or percutaneous estradiol showed no increase or decrease in the risk of breast cancer compared to synthetic progestins for at least 4 years of treatment [22] and even after 8 years [23]. Although the results

• Our recent QTL mapping study revealed that

  2020-12-11

  

  Our recent QTL mapping study revealed that the adaptor genes, including the NCK genes and the ABI genes, are located within the genomic regions harboring the most significant QTL (Zhou et al., 2017), suggesting that these genes could be involved in the determination of resistance, and possibly throu

• TUG 891 br Rationale and hypothesis To discover an allosteri

  2020-12-11

  

  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

• br Analytical improvements Since our review

  2020-12-11

  

  Analytical improvements Since our review of “Oxysterol Metabolomes” in 2011 [7], there have been a number of improvements in analytical methods for the analysis of oxysterols and related compounds. McDonald and colleagues in Dallas have refined their LC-MS methods which are now applicable for ana

• br Conflicts of interest br Financial support NZ is

  2020-12-10

  

  Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818

• While a number of studies have

  2020-12-10

  

  While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub NPPB specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing substrate u

• In plants SUMOylation has been shown to modulate

  2020-12-10

  

  In plants, SUMOylation has been shown to modulate plant hormone signaling (Lois et al., 2003, Miura et al., 2009, Conti et al., 2014), root stem cell maintenance (Xu et al., 2013), and responses to abiotic and biotic stress (Lois, 2010). Many of the plant biological processes regulated by SUMOylatio

• SIRT has deacetylated regulation on

  2020-12-10

  

  SIRT1 has deacetylated regulation on numerous nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016) to play a key role in protecting against cell stress. Therefore, the role of SIRT1 in fluorine-induced oxidative stress was explored. The results reveal

• br Are incretins the only

  2020-12-10

  

  Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr

• br Anti inflammatory effects of MTX In addition to cytotoxic

  2020-12-10

  

  Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph

• RDH belongs to C family of the short

  2020-12-10

  

  RDH10 belongs to 16C family of the short-chain dehydrogenase/reductase (SDRs) superfamily of proteins [12], [13]. Notably, in human genome adjacent to the gene encoding RDH10 on chromosome 8 are located two other genes encoding members of the SDR16C family: retinol dehydrogenase epidermal 2 (RDHE2,

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