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br Lung cancer cell lines The greatest expression of
2021-11-04
Lung cancer cell lines The greatest expression of both human and rodent FFA4 transcript has been shown to be localized to the lung [61], yet the physiological role in this tissue has been understudied, as has its involvement in lung cancers. In 2015, a two-staged genome-wide association study of
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In stark contrast to this study Zhang
2021-11-04
In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC fructose 1 6 bisphosphatase treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment
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br General features of FGFRs and
2021-11-04
General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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The ability of GPX and other
2021-11-04
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face o
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The binding of DHAP to aldolase resulted
2021-11-04
The binding of DHAP to aldolase resulted in a dramatic decrease of aldolase affinity to FBPase – KAapp was reduced more than 100 times. The dependence of the complex activity versus increasing DHAP concentration was biphasic (Fig. 3a). Supposedly, the first phase of the curve represents the state in
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PKI-402 br Introduction Thrombosis is one of the leading cau
2021-11-04
Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable PKI-402 and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–2 pe
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Senger et al performed a
2021-11-04
Senger et al. performed a retrospective review of 17 patients with ICH on dabigatran or rivaroxaban who received 4F-PCC. Eight patients had a traumatic Biotin-tyramide injury (TBI) and nine patients had a spontaneous ICH. Nine patients had a devastating outcome, including severe neurologic deficits
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Compounds and were evaluated for their pharmacokinetic
2021-11-04
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure
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It is important to mention that the IC of cetirizine
2021-11-04
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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To efficiently develop bioactive ligands even if
2021-11-04
To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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The rationale for developing HDACi as
2021-11-03
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Cyclosporin A arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematol
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Several recent studies have linked clock
2021-11-03
Several recent studies have linked clock function with the cell cycle and reported that clock components, such as PER1, PER2, BMAL1, and CRY1/2 decrease cell proliferation or improve the action of anti-cancer drugs in different cancer cell lines. Moreover, certain types of human cancer show an alter
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In an effort to further improve the intrinsic potency we
2021-11-03
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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A common principle to ameliorate underquantification because
2021-11-03
A common principle to ameliorate underquantification because of primer or probe mismatching is to employ multiple targets for detection or quantification of blood borne viruses [14]. Dual targeting real time PCRs have become common for quantification of HIV-1 [15], [16]. In a recent paper arguing fo
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br Discussion Using HBV transgenic
2021-11-03
Discussion Using HBV transgenic mice, Kim, et al. first reported that the HBx gene caused HCC [34]. Since then, transgenic mice have become a useful experimental model for defining the molecular events of HBV hepatitis, and HBV-related hepatocarcinogenesis. In the present study, we first confirme
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