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Nicastrin is heavily glycosylated contributing KDa to the
2021-11-23

Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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Over the last decade intense
2021-11-22

Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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In an effort to more fully
2021-11-22

In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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br Conclusion Leukocytes adhesion to
2021-11-22

Conclusion Leukocytes adhesion to endothelial cells is one of the most critical event in the inflammatory response. In presented paper using a relevant model of adhesion we have demonstrated that histamine influence eosinophils adhesion to endothelium. This effect appears to be mediated by H4 his
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Introduction As a compound class histone deacetylase inhibit
2021-11-22

Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic g15 mg or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3]; romidepsin (RD)
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One of the possibilities of HO targeting is gene therapy
2021-11-22

One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing SMER 3 but also have very limited i
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br Conclusion The addition of
2021-11-22

Conclusion The addition of That means to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bonds while
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br Future perspectives sGC signaling is
2021-11-22

Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com
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br STAR Methods br Acknowledgments Anthony Koleske is thanke
2021-11-22

STAR★Methods Acknowledgments Anthony Koleske is thanked for helpful discussions and for providing p190RhoGAP-A cDNA. Anatoly Kiyatkin and Mark Lemmon are thanked for use of the BioTek Synergy 2 plate reader for the MANT assays. Leena Kuruvilla is thanked for assistance with the thermal shift a
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sesamin br STAR Methods br Acknowledgments Anthony Koleske i
2021-11-22

STAR★Methods Acknowledgments Anthony Koleske is thanked for helpful discussions and for providing p190RhoGAP-A cDNA. Anatoly Kiyatkin and Mark Lemmon are thanked for use of the BioTek Synergy 2 plate reader for the MANT assays. Leena Kuruvilla is thanked for assistance with the thermal shift a
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Targeting MCTs is likely to have
2021-11-22

Targeting MCTs is likely to have dramatic effects on lactate-dependent metabolic symbiosis described in the previous paragraphs. A plethora of MCT inhibitors have been described, including α-cyano-4-hydroxycinnamate (CHC) [59], organomercurials [60], stilbene disulfonates [60], and other second-gene
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GPR A a G protein coupled receptor located mainly on
2021-11-22

GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic SKI-606 [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated i
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(R)-(-)-Niguldipine hydrochloride br Introduction Few decade
2021-11-22

Introduction Few decades after of HIV/AIDS diagnosis, it has been still a health problem and impact will continue in the next decades. In 2015, HIV/AIDS was the 12th cause of death in the world and it's estimated that 1.2 million people was died of HIV/AIDS this year. In the global epidemiologica
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Hepatic drug metabolizing enzymes and transporters expressio
2021-11-22

Hepatic drug-metabolizing trpv1 and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear receptors a
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br Acknowledgements Supported by the
2021-11-22

Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t
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