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High throughput screening HTS of the AstraZeneca compound co
2021-01-28
High throughput screening (HTS) of the AstraZeneca Bedaquiline receptor collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52
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To determine direct DDR binding
2021-01-28
To determine direct DDR1-binding partners and to further connect to Akt and mTOR signaling, we performed mass spectrometry on DDR1 immunoprecipitates and found various candidates of the Akt and mTOR pathway such as LARP1 (La-related protein 1) and RPS6 (40S ribosomal protein S6/ S6). Most intriguing
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WEHI-539 hydrochloride Studies of LRRK tagged with green flu
2021-01-28
Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the WEHI-539 hydrochloride of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defi
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The study reported here had the primary
2021-01-28
The study reported here had the primary goal to compare the methylation of HPV late genes with methylation of the DAPK promoter, and with histological or cytological diagnoses among high-risk patients that were referred to a colposcopy clinic based on abnormal cervical cytology. Based on the literat
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br Materials and methods br Results
2021-01-28
Materials and methods Results Discussion Cysteine proteases are upregulated under oxidative stress and play an important role in the preservation of cellular metabolism (Usui et al., 2007). Cysteine proteases are also important under abiotic stresses for plants to degrade proteins denatured
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Considering all these facts in the present study
2021-01-27
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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First of all two assumptions just as in Ref are
2021-01-27
First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the Calcipotriol mg of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is equal to axia
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Our results demonstrate that pt PGE
2021-01-27
Our results demonstrate that 17-pt-PGE2 - in addition to its described effects on EP1 and EP3 receptors - also acts as an EP4 agonist and thereby enhances vascular barrier function. Materials and methods Results Discussion In this study we demonstrate that the purported EP1/EP3 receptor ag
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Also our data from this study indicate
2021-01-27
Also, our data from this study indicate that gestational GC exposure altered hematological and hemorheological parameters, however reports exist that altered blood rheological markers are associated with atherosclerosis and CVD (Tzoulaki et al., 2007). Also, the platelet to lymphocyte ratio (PLR) ha
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br Biological roles of DGK br Summary and future
2021-01-27
Biological roles of DGKϵ Summary and future perspectives The most fk506 segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheless, the sequence in this segment of DGKϵ is
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Our previous studies have demonstrated that the DDR
2021-01-27
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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Safingol Alvocidib flavopiridol is a piperidine chromenone h
2021-01-27
Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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br Materials and methods br Results br Discussion In
2021-01-27
Materials and methods Results Discussion In this study, we investigated two novel candidate therapeutics, the related CRM1-inhibiting SINEs KPT-185 and KPT-276, in treatment of NHL. The results showed that KPT-185 induced growth inhibition, cell-cycle arrest, and apoptosis in tumor ddr1 rec
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br Acknowledgments This work was funded by
2021-01-27
Acknowledgments This work was funded by the EU ERDF and the Spanish Ministry of Economy and Competitiveness (MINECO) under Project TIN2013-41576-R, and the Spanish Ministry of Education, Culture and Sport (MECD) under a FPU grant (AP2010-3259), and the Andalusian Regional Government (Spain) under
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Fermentation process for growth of E coli BL DE pBMS
2021-01-27
Fermentation process for growth of E. coli BL2(DE3)/pBMS–P3Hcys was carried out in 25- and 380-L fermentors containing 15- and 250-L medium, respectively. Cell yield of about 100g/L (wet cells) was achieved by feeding glycerol and Hy-yest during fermentation. Typical fermentation parameters are show
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