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Gliptins have become a part
2020-02-21
Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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br Role of ALDH Isoenzymes in Glioma Growth
2020-02-21
Role of ALDH Isoenzymes in Glioma Growth and Invasion ALDH family genes are commonly upregulated in gliomas, indicating ALDH-dependent cell metabolism. Specific ALDH isoenzymes have been detected in high- and low-grade tumors implicated in cell proliferation, maintenance of CSC properties, invasi
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For a physiologically relevant interaction
2020-02-21
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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p is a tumor suppressor gene that inhibits cyclin
2020-02-21
p16 is a tumor-suppressor gene that inhibits cyclin-dependent kinase 4 and 6 activities and arrests the GANT 58 in the G1 phase. Aberrant methylation and mutation of p16/MTS1 in OSCC of patients was found in our previous study. Moreover, the frequency of hypermethylation of p16 from the present stud
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br Materials and methods br Results br
2020-02-21
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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br Results br Discussion Cell responds to fluctuating enviro
2020-02-21
Results Discussion Cell responds to fluctuating environmental factors by activating a set of compensatory mechanisms including changes in the lipid profile. Compensatory reactions occurring in membranes in response to phosphate deprivation include replacement of phospholipids by phosphorus-fre
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SIRT is a representative member of Sirtuins which is
2020-02-20
SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p
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In conclusion as illustrated in Fig G
2020-02-20
In conclusion, as illustrated in Fig. 5G, in response to MNNG-induced DNA damage, PARP-1 appears to have dual roles in determining the cell fate in response to MNNG: PARP-1 activation is the cause of non-apoptotic cell death via ATP depletion and PARP-1 activation is able to elicit a self-protective
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CDK S phosphorylation status influences the differential
2020-02-20
CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro
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Recently we have observed that pharmacological PPAR and PPAR
2020-02-20
Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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The generation of ROS in addition
2020-02-20
The generation of ROS, in addition to eliciting oxidative stress, is an important proapoptotic signal (Ott et al., 2007). Apoptosis is clearly associated with the production of ROS, since ROS generation occurs in the mitochondrial respiratory chain and disturbs mitochondrial homeostasis, which plays
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Here we discuss implications of
2020-02-20
Here, we discuss implications of several major families of RING-type E3 ubiquitin ligases (MDM, Cullin, GRAIL, TRAF, TRIM) as targets in inflammation and immunity, and provide insights into potential small molecule interventions to mediate the cellular responses (summarized in Table 1). We briefly c
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Here we uncover a highly
2020-02-20
Here we uncover a highly diverse superfamily of self-replicating MGEs, dubbed pipolins, which are present in three major bacterial phyla, as well as in mitochondria, and encode divergent PolB carrying TPR1 and TPR2 subdomains. Biochemical characterization of a representative enzyme encoded by a pipo
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In this study using REMD with the crystal
2020-02-20
In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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WM-1119 Preparation of the regioisomeric pyridooxazepinones
2020-02-20
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and WM-1119 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mixtu
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