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We next focused our design building into
2020-12-08

We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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During the past three decades platinum
2020-12-08

During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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For the SAR optimization of the right hand side it
2020-12-08

For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic AACOCF3 moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by condensatio
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br Introduction The discoidin domain receptors DDRs DDR and
2020-12-08

Introduction The discoidin domain receptors (DDRs), DDR1 and DDR2, are unique among the receptor tyrosine kinases (RTKs) in being activated by interaction with the extracellular matrix [1], [2]. Binding to triple-helical collagen is mediated by the receptor extracellular domains that include an N
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br Proteases with special focus on
2020-12-08

Proteases with special focus on cysteine proteases Vaccination using cysteine proteases as antigens with special emphasis on DNA-vaccines Concluding remarks In spite of the great potential of DNA vaccines, the technology has not been as revolutionary as expected in higher mammals. In fish,
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Distribution of DGTS in basidiomycete fungi
2020-12-08

Distribution of DGTS in basidiomycete fungi has been demonstrated to be heterogeneous. In certain fungal taxons, such as Agaricales, Polyporales and Russulales, there are species that synthesize and species that do not synthesize DGTS that belong to the same order or even family (Dembitsky, 1996, Va
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The majority of pro inflammatory cytokines are regulated by
2020-12-08

The majority of pro-inflammatory cytokines are regulated by NFκB, and recently, it has been found that p38 MAPK partly regulates NFκB-driven gene Ro3306 by increasing the association of the basal transcriptional factor, TATA-binding protein, with the C terminus of p65 subunit of NFκB and increasing
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NPC L NPC Niemann Pick C like like
2020-12-08

NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol GW788388 from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cholesterol-lower
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Thus the understanding of the various mechanisms
2020-12-07

Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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br Methods br Results Main characteristics of study
2020-12-07

Methods Results Main characteristics of study population are presented in Table 1. AD cases had higher co-morbidity score and lower socioeconomic position than controls. Women with AD had undergone any surgery (unilateral/bilateral oophorectomy, hysterectomy, hysterectomy with bilateral oophor
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br Acknowledgements Professor Olli A
2020-12-07

Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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Upon assembly of HLA tetramers loaded
2020-12-07

Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T Azithromycin recognizing the respective peptide-HLA complexes. We found no significant difference in frequencies
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Human neutrophil elastase HNE is
2020-12-07

Human neutrophil elastase (HNE) is a serine protease central to the pathology in a wide range of diseases including chronic wounds, cystic fibrosis, and acute respiratory distress syndrome (Owen, 2008). Although neutrophil proteases are necessary for completion of wound healing, HNE is secreted in h
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br Materials and methods br Results br
2020-12-07

Materials and methods Results Discussion Oxidative stress is a disturbance in the balance of pro- and antioxidant species, resulting in oxidative damage to membrane proteins, lipids, and DNA. Oxidative stress is a predisposing factor for the progression of metabolic diseases and liver injur
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Crystallographic and NMR based analyses have revealed that R
2020-12-07

Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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