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Ung et al examined a variety of structural features
2020-04-09

Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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Cilengitide Introduction Maintenance of genome integrity is
2020-04-09

Introduction Maintenance of genome integrity is essential for life, and faithful DNA replication and repair ensure this. One of the most important parameters for DNA maintenance is the regulation of optimal concentrations of the four 5′-deoxyribonucleoside-triphosphates (dNTPs) the precursors for D
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br Acknowledgments This work was supported
2020-04-09

Acknowledgments This work was supported by Natural Science Foundation of China (No: 81501485). We are particularly grateful to Dr. Dan Yang and Dr. Yi Zhang for their assistance and facilities in helping this experiment and manuscript. Oral squamous cell carcinoma (OSCC), the most common malig
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br Experimental section br Notes br PDB ID codes
2020-04-08

Experimental section Notes PDB ID codes The atomic coordinates and structure factors of hDHODH in complex with compounds 4 (PDB id: 5MVC), 5 (PDB id: 5MVD) and 6 (PDB id: 5MUT) have been deposited in the RCSB Protein Data Bank. Acknowledgements This research was financially supported by
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Erlotinib Hydrochloride receptor Our previous work has demon
2020-04-08

Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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The small intestine in addition to its primary
2020-04-07

The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 Imiloxan hydrochloride present in the liver are also present in the small intestine althou
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GLP signaling mediates important renal functions
2020-04-07

GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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We have compared the potency of a series of DNA
2020-04-07

We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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br Diacylglycerol kinases and T cell responses br Diacylglyc
2020-04-07

Diacylglycerol kinases and T cell responses Diacylglycerol kinases and cancer Several studies implicate DGKα in tumor progression, but its function is debated, as it might also have roles as a tumor suppressor. Diminished DGKα expression is linked to malignant transformation in epithelia. High
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It is not precisely known which of the intramolecular
2020-04-07

It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH3
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Several reasons may explain that other studies using PDE
2020-04-07

Several reasons may explain that other studies using PDE-5-Is yielded negative or contradictory results [30], [31], [32]. Lee [30] applied 50mg sildenafil to seven patients with liver cirrhosis. NO and cGMP in the hepatic JSH-23 significantly increased, hepatic and pulmonary resistance decreased,
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A particularly important system in which Eph ephrin
2020-04-07

A particularly important system in which Eph-ephrin signaling has been widely studied is neural development, in which downstream signal transduction controls neural stem cell (NSC) proliferation, migration, and survival both during early development and in adulthood (19, 20, 21). Furthermore, Eph-ep
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The imaging and biochemical data presented here
2020-04-07

The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a
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Although enantioselective accumulation of metalaxyl in organ
2020-04-07

Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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In contrast to SQLE HMGCR could
2020-04-07

In contrast to SQLE, HMGCR could be efficiently degraded in hdac inhibitors lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our re
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