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The optimization of the lead compound was initiated and the
2020-10-23

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 Betaine moiety with other functional groups led to loss of functional activity against EP4 receptor. Alt
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More than thirty enzymes with PLA activity
2020-10-23

More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos
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A structural explanation for how RBR RING
2020-10-23

A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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Published results have revealed relationships between serine
2020-10-23

Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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As previously stated the most unexpected finding from
2020-10-23

As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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VRT752271 mg Michel et al calculated the mutual
2020-10-23

Michel et al. [34] calculated the mutual solubilities of water and hydrocarbons by a cubic equation of state. They asserted that conventional mixing rules can not satisfactorily describe the hydrogen bonding compounds. Kabadi and Danner [35] applied a modified form of Soave-Redlich-Kwong equation of
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br Disclosures br Introduction The presence of
2020-10-23

Disclosures Introduction The presence of anti-viral T-cell immunity is crucial for effective and sustained protection against Cytomegalovirus (CMV) following allogeneic stem cell transplantation (alloSCT) [1]. In vitro and in vivo T-cell depletion (TCD) via addition of the anti-CD52 monoclonal
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Gene expression profiling with corresponding
2020-10-23

Gene HPF synthesis profiling with corresponding clinical data supported the notion that increased expression of S1PR1 in DLBCL was associated with poor outcome [159], [160], [161]. These studies also identified increased expression of the GPCRs GPR183, CCR7, ADRB2 and CNR2 as risk factors for poor o
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br Most reported binding data
2020-10-22

Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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Since clinical studies mostly involved cases
2020-10-22

Since clinical studies mostly involved cases that used MPA, data from studies that examined other types of progestogens are very limited. While the WHI study examined the combination of conjugated equine estrogens plus MPA [1], the Million Women Study [2] that also demonstrated an increased risk of
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Tolvaptan br Materials and methods br Results br
2020-10-22

Materials and methods Results Discussion Our previous study showed that ERRγ negatively regulates osteoblast differentiation via inhibiting Runx2 transactivity (Jeong et al., 2009). In the present study, we found that ERRγ also induced miR-433 in osteogenic mesenchymal cell lineage C3H10T1/
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Early VL diagnosis makes it
2020-10-22

Early VL diagnosis makes it possible to formulate a quicker and more effective treatment against the disease, which could increase the possibility of a cure for the patients, as well as reduce the toxicity of the drugs (Coelho et al., 2009); however, conventional and molecular parasitological method
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Keratin K has been identified as the first
2020-10-22

Keratin 8 (K8) has been identified as the first intermediate filament expressed during development in amphibians and mammals. In zebrafish, a type II cytokeratin 8 (zf-K8) cDNA has been cloned. zf-K8 gene was maternally inherited and expressed in all surface cells throughout the embryonic stages old
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The study reported here had the
2020-10-22

The study reported here had the primary goal to compare the methylation of HPV late genes with methylation of the DAPK promoter, and with histological or cytological diagnoses among high-risk patients that were referred to a colposcopy clinic based on abnormal cervical cytology. Based on the literat
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br Expression and Purification of Atg and
2020-10-22

Expression and Purification of Atg4 and Atg8 Proteins for In Vitro Assays Measurement of Atg4 Activity In Vitro and Ex Vivo Kinetics Analysis of Atg4 Enzymes Summary Atg4 proteases play a crucial role in preparing Atg8 for conjugation to lipid membranes and for the deconjugation of Atg8
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