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The optimization of the lead compound was initiated
2020-10-30
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Concanamycin A moiety with other functional groups led to loss of functional activity against EP4 recept
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Omar Farha and coworkers have recently successfully
2020-10-30
Omar Farha and coworkers have recently successfully employed metal-organic frameworks (MOFs) to tackle these limitations while retaining the essential characteristics of an immobilization material. MOFs consist of metal ions, or small clusters thereof, coordinated with organic ligands. MOFs are high
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Introduction The number of patients
2020-10-30
Introduction The number of patients with type 2 diabetes is increasing globally, and has become a serious public health problem. Type 2 diabetic patients exhibit a higher risk of bone fracture [1]. In addition, clinical studies have indicated that increased fracture risk is associated with long-ter
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The other interesting observation made during
2020-10-30
The other interesting observation made during this study relates to the differences between the discrete IR-induced γH2AX foci and the robust H2AX phosphorylation observed during apoptotic DNA fragmentation. The pattern of H2AX phosphorylation observed during DNA fragmentation possibly reflects the
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Iris domestica L Goldblatt Mabb
2020-10-30
Iris domestica (L.) Goldblatt & Mabb. (syn. Belamcanda chinensis L.) DC. (Iridaceae) occurs naturally in South and East Asia. Despite the fact that former monotypic genus Belamcanda has been included in the extended genus Iris, this classification has been questioned (Wilson, 2011; Mavrodiev et al.,
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Next we compared the protease specificity
2020-10-30
Next, we compared the protease-specificity of viruses NS116-GFP/AE and NS116-GFP/AT for trypsin, neutrophilic elastase or supernatant of human neutrophils. For later purposes, we determined the viral yield in a co-cultivation system of infected Vero fura 2 with human neutrophils. The NS116-GFP/elast
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br Signaling of DDR receptor and its regulation Being
2020-10-30
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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Although BPA has been proven to
2020-10-29
Although BPA has been proven to cause many health issues such as obesity and neurological toxicity (Rubin, 2011), the effects and mechanisms of BPA on the human tumorigenesis and cancer development are still not well illustrated. In the present study, we found that 10 to 10M BPA significantly promot
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Structure similarity searches were conducted
2020-10-29
Structure similarity searches were conducted using the standalone version of the DALI program with the query structures scanned against a local current version of the PDB that has all chains as separate entries (Holm and Sander, 1995). The structural hits for each query were collected, even if the D
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br Common features of TdT
2020-10-29
Common features of TdT, pol μ and pol λ TdT, pol μ and pol λ remain in a closed conformation throughout their catalytic cycle, contrary to pol β [24•, 53, 54•]. One possible explanation for this observation is that they have traded fidelity (which requires open-to-closed transition) for a very ti
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Mitochondrial depolarization induced by DHODH inhibition Fig
2020-10-29
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Numerous studies have pointed to the DGAT
2020-10-29
Numerous studies have pointed to the DGAT reaction being critical for TAG assembly and in several cases it has been shown to limit carbon flux from lipid precursors towards TAG accumulation [12]. Thus, in Brassica napus, the DGAT substrate, diacylglycerol (DAG), accumulates during periods of rapid l
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br Materials and methods br Results br Discussion Recently
2020-10-29
Materials and methods Results Discussion Recently, circRNAs have been found to play important diagnostic or prognostic roles in different tumors. For example, aberrant expression levels of different circRNAs are found in ovarian cancer, lung cancer, renal cancer, gastric cancer and particip
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Here we examine the associations between
2020-10-29
Here, we examine the associations between serum pro and anti-inflammatory cytokines and cognitive functioning in early-stage bipolar I disorder (BDI) patients. As per previous studies, ‘early-stage’ was defined as being within three years of the first manic episode (Kauer-Sant\'Anna et al., 2009). W
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Imiquimod hydrochloride br Conflict of interest statement br
2020-10-29
Conflict of interest statement Acknowledgement The study was financially supported by the Ministry of Education, Youth and Sports of the Czech Republic – projects “CENAKVA” (No. CZ.1.05/2.1.00/01.0024) and “CENAKVA II” (No. LO1205 under the NPU I program), by the Grant Agency of the University
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