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The data presented here support a dynamic and complex interp
2021-09-09
The data presented here support a dynamic and complex interplay among labile heme, BACH1 and HO-1. It appears also that metabolites of heme degradation may participate in the mechanistic regulation of the various factors examined. Our results point to the possibility that the HO-1 pathway restricts
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br Background To treat chronic HCV
2021-09-09
Background To treat chronic HCV genotype (GT) 1-infected patients, telaprevir (TLP) or boceprevir (BOC), first generation protease inhibitors (PIs), were used in combination with pegylated-interferon (PEG-IFN) and ribavirin (RBV) triple therapy [1], [2]. The main weaknesses of the first-generatio
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For the SAR study human haspin kinase inhibitory activity
2021-09-09
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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Mortality from breast cancer is almost always attributed to
2021-09-08
Mortality from breast cancer is almost always attributed to metastatic spread of the disease to other organs, thus precluding resection as a treatment method. Unfortunately, conventional chemotherapy fails to eradicate most human cancers, including aggressive breast cancers. Studies over the past de
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br Introduction Opioids have long been used in pain
2021-09-08
Introduction Opioids have long been used in pain management [1]. However, their non-medical use has grown rapidly in the last few years. Hydrocodone (HYD) is one of the most widely used short-acting opioids; with over 136.7 million prescriptions in 2011 [2]. HYD is a semi-synthetic opioid used fo
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br Introduction Maintaining blood glucose
2021-09-08
Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The (R,S)-Anatabine sale is especially dependent on an adequate, continuous supply of circulating gl
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Retinal GAL receptor distribution suggests
2021-09-08
Retinal GAL receptor distribution suggests an intrinsic neuronal control since retina lacks an autonomic innervation, and a signal modulation seems most likely here, acting via GALR1 while GALR2 and GALR3 seem to play a rather minor role in this signal transduction. While sources acting on these ret
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The highest metabolic stability observed for
2021-09-08
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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Murine models of AML were used to identify
2021-09-07
Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia tgf beta inhibitor arrest through regulation of cyclin-dependent kinases and increased expressi
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This study was supported by the Finance Department Foundatio
2021-09-07
This study was supported by the Finance Department Foundation of Jilin Province (3D5178963428). Introduction Breast cancer is one of the leading cause of death in women worldwide [1,2]. Due to recent advances of combined therapies, survival rate of breast has improved significantly. However, bre
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br Hepatitis C virus HCV infection is
2021-09-07
Hepatitis C virus (HCV) infection is a major cause of chronic liver disease that can lead to cirrhosis and hepatocellular carcinoma. It is estimated that nearly 200 million individuals worldwide are currently infected with HCV and it is the leading cause of liver transplants. The current standard
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br Methods br Results br Discussion Our results show that
2021-09-07
Methods Results Discussion Our results show that the DRG and the spinal cord express significant amount of GPR35, a previously orphan Gi protein coupled receptor whose stimulation with zaprinast or with KYNA may reduce inflammatory pain. The receptor is also expressed in primary cultures of
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The atherosclerosis development requires additional pro infl
2021-09-07
The atherosclerosis development requires additional pro-inflammatory response in the vascular tissue, promoting increased levels of adhesion molecules such as VCAM-1 (vascular cell adhesion molecule-1) and ICAM-1 (intercellular adhesion molecule-1). Cytokines such as TNF-α and IL-1β are able to upre
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It is well known that O tetradecanoylphorbol acetate
2021-09-07
It is well known that 12-O-tetradecanoylphorbol-13-acetate (TPA) is a tumor promoting agent of skin carcinogenesis in rodents [12]. TPA stimulates a variety of cellular functions in cancer cells, including cell motile activity [13], [14]. In our recent study, when liver epithelial cells were treated
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The post translational modification O GlcNAcylation is
2021-09-07
The post-translational modification O-GlcNAcylation is also dependent upon glucose fluctuations. O-GlcNAcylation has been linked to insulin resistance and glucose toxicity in diabetes and its comorbidities [11]. O-GlcNAcylation is a dynamic modification tightly regulated by the nutritional sensor UD
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