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The quantification and monitoring of ChEs enzymatic activiti
2021-04-07

The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c
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An ideal CHK inhibitor would
2021-04-07

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
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br Author contributions br Funding M E
2021-04-07

Author contributions Funding M.E.B. was supported by Research Fund #3096. Competing interests Introduction Lung cancer has become one of the most common death causes in both male and female malignant tumors (Jemal et al., 2011). Air pollution, smoking and estrogen level are known risk f
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It has previously been shown that human
2021-04-07

It has previously been shown that human melanocytes are responsive to a multiplicity of hormonal triggers [10], particularly to pituitary or ovarian hormones [11]. Studies concerning the effects of AGN 194310 mg on human melanocytes led to inconsistent data [12], [13]. Im et al. [14] reported that
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br Materials and methods br Results br Discussion CDK and
2021-04-02

Materials and methods Results Discussion CDK and their regulatory cyclins form a family of heterodimeric kinases that are particularly important for regulation of ESI-09 sale progression and transcription in tumor cells. These kinases therefore constitute biomarkers of proliferation and at
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br Conclusion In conclusion the current study showed that ce
2021-04-02

Conclusion In conclusion, the current study showed that central CRF signals have crucial roles in behavioral changes, such as locomotor activity and anxiety behavior. In contrast, the hormonal regulation of CRF through HPA axis can be primarily modulated at the peripheral level. CRF1 receptor ant
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Another option is to use the thiol groups
2021-04-02

Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st
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Hymenialdisine the most potent inhibitor of
2021-04-02

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this NS 11021 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK5/c
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There is a large interindividual difference in intestinal ch
2021-04-02

There is a large interindividual difference in intestinal cholesterol FG2216 of cholesterol that is mainly due to genetic variation [15], [19]. Single nucleotide variation (SNV) in NPC1L1 and, ABCG5 and ABCG8 key modulators of cholesterol influx and efflux into intestinal mucosal cells, respectivel
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The transcription factor CREB has
2021-04-01

The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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br Regulation of cadherin switching The downregulation of E
2021-04-01

Regulation of cadherin switching The downregulation of E-cadherin during cadherin switching is induced by multiple mechanisms, including methylation of the E-cadherin promoter and signaling pathways that activate E-cadherin-suppressing transcription factors [[61], [62], [63]]. During the progress
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br E E backside interaction The
2021-04-01

E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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Next we evaluated whether DPP inhibitor suppressed osteoclas
2021-04-01

Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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In studies directed toward the development of sequence speci
2021-04-01

In studies directed toward the development of sequence-specific major-groove binding small TCS 2002 [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and af
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Next the BE obtained for the different complexes
2021-04-01

Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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