• It has been reported that expression of murine haspin is

  2021-12-29

  

  It has been reported that expression of murine haspin is found only in post-meiotic spermatids and that overexpression of murine haspin in HEK-293 cells leads to reduced cell proliferation. Therefore, it was suggested that haspin functions to bring about casin arrest in haploid germ cells (Tanaka e

• Under most circumstances NO is a potent endogenous vasodilat

  2021-12-29

  

  Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response

• Racemic protein crystallography has been proven to be a powe

  2021-12-29

  

  Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,

• Despite the association with asthma it is not surprising

  2021-12-29

  

  Despite the association with asthma, it is not surprising that we did not find a relation between the percent predicted FEV1 and SNPs in GSNOR. FEV1 measured on a routine clinic visit is likely to be normal in most asthmatic children. FEV1 in children reflects a complex mix of factors in the growth

• Selective pharmacological inhibition of tonic currents indic

  2021-12-29

  

  Selective pharmacological inhibition of tonic currents indicated that the effects of gp120 are predominantly mediated by α5-containing GABAARs. The other dominant subtype that contributes to tonic current in the hippocampus, the δ-containing GABAAR, was unaffected by gp120 treatment. Additionally, i

• Generally speaking the regulation of GnIH on gonadotropins s

  2021-12-29

  

  Generally speaking, the regulation of GnIH on gonadotropins synthesis and release, although controversial, could be direct and/or indirect via GnRH, among others peptides. In this sense, different scenarios have been reported in vertebrates. In mammalian and avian species, GnIH fibers reach the med

• In silico analysis revealed structural

  2021-12-29

  

  In silico analysis revealed structural similarities between the CpMutY and the EcMutY which share typical domains and structural motifs (Fig. 5), common to a wide range of structurally related DNA repair enzymes. These include an endonuclease III domain, involved in excision of damaged pyrimidines,

• br Conclusions and future perspectives br Declarations of in

  2021-12-28

  

  Conclusions and future perspectives Declarations of interest Acknowledgements The authors thank Mrs. Kamala Pandey for the help in the preparation of this manuscript. This work was supported by NIH grants R01HL057531 and R01HL062147. Introduction Separation of short exons by long non-co

• Since TgGC resisted several knockout attempts with CRISPR Ca

  2021-12-28

  

  Since TgGC resisted several knockout attempts with CRISPR-Cas9, we utilized traditional epitope tagging and an auxin-inducible degron (AID) system (Brown et al., 2017, Brown et al., 2018, Long et al., 2017) to detect and regulate TgGC expression. TgGC localizes to the apical cap region of the plasma

• Because of its excellent GPR potency good hERG selectivity

  2021-12-28

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Butyrolactone 3 synthesis was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an ext

• Curcumin is the active ingredient extracted from the natural

  2021-12-28

  

  Curcumin is the active ingredient extracted from the natural medicine turmeric rhizome (Goel et al., 2008, Aggarwal and Harikumar, 2009). Studies have shown that curcumin has anti-tumor, anti-inflammatory, antioxidant and antimicrobial properties (Larsen et al., 2007, López-Lázaro, 2008). Although c

• In addition to inactivation of Notch

  2021-12-27

  

  In addition to inactivation of Notch, we found that the combination of BTZ and GSI-I downregulated ERK phosphorylation in ALK+ ALCL cells, and we speculate this may occur through the inhibition of upstream regulators of the ERK pathway. These findings emphasize the functional complementation of the

• Optimization of the tetrahydroindazole series led

  2021-12-27

  

  Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ().

• br Results and discussion br Conclusion In the continued

  2021-12-27

  

  Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by Sorbitol 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaffolds, the

• br FGF FGFR pathway as predictive factor Several

  2021-12-27

  

  FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m

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