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The swelling independent activation of chloride channels by
2020-11-11
The swelling-independent activation of chloride channels by glycerol is proved by our further experiments. When glycerol concentration in the isoosmotic solution was reduced to the micromolar scale or even lower concentration, a Cl− current was still induced. The ap-1 were not swollen by these trea
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Chk is dramatically induce by the
2020-11-11
Chk is dramatically induce by the IL-4 family of cytokines and equally dramatically inhibited by IFN-γ, a regulation that appears to be specific for human monocytes. In primary human T cells, Chk is not normally present, but it can be induced by potent activators of T Argatroban sale such as PHA or
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Several CHK inhibitors have been reported
2020-11-11
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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Therapeutic options targeting intrahepatic resistance are ve
2020-11-11
Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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Together the data suggests that more work needs
2020-11-11
Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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br The orphan estrogen related
2020-11-10
The orphan estrogen-related receptor exists as three subtypes (ERRα, ERRβ, and ERRγ) in the human genome. ERRα is expressed in metabolically active tissues such as muscle and adipose. ERRγ is expressed in the spinal cord and CNS. ERRβ appears to play a role in development, as postnatal expression
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Given the potency enhancing effect of the butyl
2020-11-10
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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br Materials and methods br Results
2020-11-10
Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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In the present study promoting bile acid synthesis by
2020-11-10
In the present study, promoting bile 5-Ethynyl-2'-deoxyuridine synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for
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br Materials and methods br Results We examined the effects
2020-11-10
Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 salidroside stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2+ levels
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The redox sensitive transcription factor
2020-11-10
The redox sensitive transcription factor NF-κB is reported to play a crucial role in the COPD pathogenesis via up regulating the expression of several cytokines, chemokines, growth factors, and adhesion molecules [71]. Incidentally, we and others have shown that PARP-1 modulates the NF-κB activation
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Herbal products may alter the metabolism of
2020-11-10
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 SJB3-019A mg (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological ac
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br Marginal zone lymphoma Marginal zone lymphoma MZL compris
2020-11-10
Marginal zone lymphoma Marginal zone lymphoma (MZL) comprises three lymphoma entities that arise from the marginal zone surrounding the germinal center: extranodal MZL or mucosa-associated lymphoid tissue (MALT), splenic MZL, and nodal MZL. Deep sequencing of nodal MZL patients found that 5/35 (1
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br The classical ubiquitination pathway Ubiquitination is an
2020-11-10
The classical ubiquitination pathway Ubiquitination is an enzymatic process that involves the addition of an ubiquitin protein to a substrate that usually becomes inactivated followed by degradation in the proteasome; however, several other functions have also been described. For the discovery of
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Our study provides proof of principle for dimerizing
2020-11-10
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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