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While previously reported optimizations on compound
2021-07-29
While previously reported optimizations on Calpain Inhibitor XII focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to exp
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Adding more pieces to the puzzle using a human to
2021-07-29
Adding more pieces to the puzzle, using a human-to-animal crossover study, blood taken from healthy volunteers that underwent exercise was used as a dialysate to perfuse a rabbit heart in a Langendorff model of MI [62]. Unprecedentedly, dialysate of plasma from exercised humans reduced infarct size
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4μ8C mg Furthermore elastase might not be the only regulator
2021-07-29
Furthermore, elastase might not be the only regulator of CBG on cleaved and uncleaved form. In a study by Nenke et al. [85] α1-AT deficient subjects, who lack this native neutrophil elastase inhibitor, paradoxically have higher levels of uncleaved CBG and lower levels of CBG* [85]. Gender differenc
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br Materials and methods br Results
2021-07-29
Materials and methods Results Discussion The investigation of oxysterols is highly complex and challenging, arising not only from the large number of molecules in this family, but also due to their low abundance in biological systems compared to cholesterol and their susceptibility for aut
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br Ubiquitination and deubiquitination pathways Ubiquitinati
2021-07-29
Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec
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Further indirect evidence supporting an
2021-07-29
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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br Conclusion The role of DNA PK target
2021-07-29
Conclusion The role of DNA-PK target in DNA DSB repair renders this JQ1 kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design of poten
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Compound was advanced to a chronic
2021-07-29
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, inno-206 sale 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured dai
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nfat receptor br Materials and methods br Results
2021-07-29
Materials and methods Results and discussion Conclusions Clitocypin is another member of the mycocypin family of cysteine protease inhibitors that is unique to nfat receptor shown to exhibit strong insecticidal activity against Colorado potato beetle larvae. This effect is concentration de
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O-propargyl-puromycin Partial suppression of the cot
2021-07-29
Partial suppression of the cot-1 (ts) phenotype by deletion of gul-1 has been well documented (Seiler et al., 2006). This is now also very clearly evident in the transcriptional profile of the various strains (Fig. 2). Furthermore, the comparative analysis of the single and double mutants revealed,
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br Introduction Phosphorus P is an important nutrient for
2021-07-28
Introduction Phosphorus (P) is an important nutrient for plant growth; however, in many regions of the world soils are low in plant-available P (Holford, 1997). Therefore, P fertilisers play an important role in agriculture. Most P fertilisers in current use are derived from phosphate rock; howev
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br Materials and methods Details on materials
2021-07-28
Materials and methods Details on materials and methods can be found in the Supplemental material section. Results Discussion In our experiments we mimicked inflammation by LPS challenge of M0 macrophages. We discovered a strong increase in expression of CH25H and CYP7B1 while CYP27A1 and H
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Lymphocyte mobility and homing is
2021-07-28
Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21
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br Multi subunit RINGs There are RING type E
2021-07-28
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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DUBs are involved in cell cycle regulation and DNA
2021-07-28
DUBs are involved in nmda regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 2010, Gupta et al., 2010), it
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