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The mechanism by which these HIV PIs impair skeletal
2021-07-22

The mechanism by which these HIV-PIs impair skeletal muscle palmitate transport and oxidation has been partially elucidated. CD36 (also referred to as fatty 3-CPMT translocase; FAT) is a transmembrane protein involved in the transport of long-chain fatty acids (LCFA) across cellular membranes. It h
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Previously published data showed an interaction of tubulin a
2021-07-22

Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino SB-334867 hydrochloride mg se
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br Conclusions br Introduction Today just as for the past
2021-07-22

Conclusions Introduction Today – just as for the past 50 years – the most commonly used repellent in the world is DEET (Fradin, 1998; Pickett et al., 2008). The active ingredient, N,N-Diethyl-m-toluamide, is an oily synthetic substance applied topically to the skin in order to alter the host f
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br Materials and methods br Results To
2021-07-22

Materials and methods Results To investigate the effect of 17βE on cell proliferation in the human renal tubular epithelia, BrdU uptake was measured in HRTEC primary and 3D-HRTEC cultures, allowing determination of the DNA replication rate. Representative microphotographs show BrdU uptake in H
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br Experiments br Numerical simulations
2021-07-22

Experiments Numerical simulations Discussion Conclusions By large-caliber PELE with various d/D against RHA plate at low velocity of 415 m s−1, impact experiments against 30 mm RHA target were carried out. Numerical simulations were also conducted to monitor progress of PELE expansion an
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Another enzyme class that has emerged
2021-07-22

Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Oxidoreductase like MEM for prodrug activation br Future
2021-07-22

Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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Human neutrophil elastase HNE is
2021-07-22

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 Author contribution br Acknowledgements We want to thank
2021-07-22

Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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PAC-1 mg br Results and discussion br Conclusion
2021-07-22

Results and discussion Conclusion Based on the structure of ThDP, in this study, a series of novel ThDP analogs 6a-6g and 8a-8g were designed by optimizing triazole-benzene linker and modifying the substituent group of triazole ring. Then they were synthesized as potential inhibitors of Cy-PDH
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br Conclusion The role of DNA PK target in
2021-07-22

Conclusion The role of DNA-PK target in DNA DSB repair renders this EPZ-6438 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
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We then undertook computational studies that suggest the cya
2021-07-21

We then undertook computational studies that suggest the cyanobacterial ALDH (and planctomyces ALDH) represent the evolutionary ancestor of human and other eukaryotic ALDH1/2 given that cfALDH contains signature residues matching both the human proteins throughout the surface of the protein and the
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During the course of our research on mGlu PAMs the
2021-07-21

During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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Recently it has been shown that among
2021-07-21

Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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Injurious effects of cigarette smoke CS on human
2021-07-21

Injurious effects of cigarette smoke (CS) on human health are progressively being acknowledged both in animal and human studies. CS is a highly complex mixture that contains substantive amounts of toxic oxidants, nitric oxide, organic compounds, free radicals and microbial cell components including
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