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Compound was prepared from chloroindole by acylation
2021-07-19
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole CHIR-124 derivative (). Derivatives and were pr
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Herbal products may alter the
2021-07-19
Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 74 synthesis (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological a
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It is particularly notable that CYP D appears to
2021-07-19
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 encorafenib in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and between i
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There is evidence that the response of CYP activity
2021-07-19
There is evidence that the response of CYP450 activity to DEX is species-specific. CYP1A and CYP3A expressions were strongly induced by DEX in porcine hepatocytes (Rasmussen et al., 2014) and in rat and human, but not minipig or beagle dog hepatocytes (Lu and Li, 2001). Within fish, there are also s
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The goal of studying RvE in goblet cells is to
2021-07-17
The goal of studying RvE1 in goblet Polymyxin B sulfate is to determine if it may be used to preserve ocular surface homeostasis and as a treatment of ocular inflammatory diseases. We found that RvE1 increased glycoconjugate secretion after 2 h, not at 4 h. This suggests that RvE1 has a short, but p
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br Authors contribution br Disclosure statement br Acknowled
2021-07-17
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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Because stimulation and blockade of
2021-07-17
Because stimulation and blockade of dopamine D2 receptor all cause a similar disruption of maternal behavior, one critical question is whether they do so through the same or different behavioral mechanisms. One idea is that stimulation or blockade of D2 receptors similarly suppresses maternal motiva
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In this report we evaluate
2021-07-17
In this report, we evaluate if this molecular mechanism is used universally by high-fidelity DNA polymerases during the replication of DNA lesions that are structurally distinct from abasic sites. This was approached by quantifying the kinetic parameters for the incorporation of modified and non-nat
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br Introduction DNA ligation is required during DNA replicat
2021-07-17
Introduction DNA ligation is required during DNA replication and to complete almost all DNA repair events. In human cells, the DNA ligases encoded by three LIG genes are responsible for joining interruptions in the phosphodiester backbone [1]. These enzymes have distinct but overlapping functions
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Our current understanding of nucleotide metabolism in has
2021-07-17
Our current understanding of nucleotide metabolism in has made it possible to identify numerous proteins which serve essential roles in the life cycle of the parasite. One such protein is thymidylate synthase-dihydrofolate reductase (TS-DHFR), a bifunctional enzyme which is necessary for the product
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br Experimental br Results and discussion br Conclusions In
2021-07-17
Experimental Results and discussion Conclusions In this work we presented the direct electrochemical behaviour of the Mo containing formate dehydrogenase, purified from D. desulfuricans, where the Mo centre redox features were observed. The results allowed to calculate the reduction potenti
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The second DDR binding partner identified
2021-07-17
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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loteprednol receptor br Materials and methods br Results The
2021-07-17
Materials and methods Results The frequency of hypermethylation of RARbeta, RASSF1A, FHIT, GSTP1, MGMT, VHL and DAPK in patients with primary LSCC was assessed in both the tumor tissue samples and macroscopically and histologically normal mucosa from distant sites of the surgical specimen, lot
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To assess which export pathway
2021-07-17
To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 BTB06584 with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well as
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A related cell based approach
2021-07-17
A related, cell-based approach was used to test the functionality of the various HIV Rev fusions, but in a trans-complementation assay using 293T producers transfected with both VSV G and a Rev-deficient HIV reporter vector encoding both FFLUC and bsd (Fig. 2C). As expected, the non-fused, full-leng
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