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We show that pharmacological inactivation of GSTP over
2022-03-18
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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To characterize the binding receptor for HIV
2022-03-18
To characterize the binding receptor for HIV-1 gp120 in autophagy, we used the CXCR4 inhibitor AMD3100 and NMDA receptor inhibitor MK801 along with gp120 to treat the cardiomyocytes. Our data demonstrated that inhibition of the NMDA receptor significantly blocked the increase of gp120 induced autoph
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DCG IV In the brain hydrolysis of AG by MGL is the
2022-03-18
In the brain, hydrolysis of 2-AG by MGL is the primary source of AA for conversion to PGs by cyclooxygenase (Nomura et al., 2011). PGE2 production is required for IL-1β-evoked synapse loss (Mishra et al., 2012). Here, we tested whether decreased PG levels contributed to the synapse protective effect
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The results of our study indicate the
2022-03-18
The results of our study indicate the general importance of the gp120 V3 loop a66 patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to gp120 shedding i
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Fmoc-Cl Our exploration of Domain focused
2022-03-18
Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be repla
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RGFP966 Heterocysts provide the required microoxic environme
2022-03-18
Heterocysts provide the required microoxic environment for the oxygen-sensitive N2-fixing nitrogenase enzyme complex. This environment is formed during heterocyst development. Developing heterocysts inactivate photosystem II and degrade antenna pigments, thereby decreasing oxygenic photosynthesis (F
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Introduction Osteoarthritis OA is a prevalent disease
2022-03-17
Introduction Osteoarthritis (OA) is a prevalent disease characterized by chronic joint degeneration, including articular cartilage loss, synovitis and osteophyte formation [1], [2], [3], [4], [5]. The cause of OA is metabolic imbalance and mechanical stress, which is coupled with inflammation, lead
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The first GSM was identified from the discovery of
2022-03-17
The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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The molecular target of N BPs
2022-03-17
The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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br Ethics statements br Introduction Hepatocellular carcinom
2022-03-17
Ethics statements Introduction Hepatocellular carcinoma (HCC) is the fifth most common malignant tumor and the third leading cause of cancer-related mortality worldwide, with rapidly-increasing incidence in recent years [1,2]. Mounting evidence shows that viral hepatitis, toxin exposure, non-a
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Fmoc-Ile-Wang resin Although the presence of histamine secre
2022-03-17
Although the presence of histamine-secreting bacteria has been well documented in foods, their presence within the human gut microbiota has not been investigated in detail. We recently performed an analysis of fecal samples from 161 volunteers to quantify the presence of bacterial HDC, using primers
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Kinases belonging to the Thousand
2022-03-17
Kinases belonging to the Thousand and one (Tao) family are conserved throughout evolution. Three Tao proteins are encoded in the human genome (TAO1, TAO2, and TAO3), while D. melanogaster possesses a single ancestral Tao kinase (Tao-1). Like Hpo and GckIII, Tao kinases belong to the Sterile 20-like
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The medicinal properties of guanidine derivatives are also
2022-03-17
The medicinal properties of guanidine derivatives are also of great interest due to their diverse anti-microbial, anti-inflammatory, anti-viral, and anti-cancer, activities (C and D). Guanidine-containing drugs, such as -iodobenzylguanidine and methylglyoxal bis(guanylhydrazone), were shown several
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br Conclusion The mitochondrial and glycolytic energy metabo
2022-03-17
Conclusion The mitochondrial and glycolytic energy metabolism of the brain is coordinated by HKI binding to MOM, although the molecular mechanism of such a regulation is not yet clear. The Rapalink-1 for HKI in MOM are VDACs [[5], [6], [7]], mainly the VDAC1 isoform [8]. Using a computational mo
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br Conflict of interest br Funding br Introduction Heme is
2022-03-17
Conflict of interest Funding Introduction Heme is an essential molecule for cellular metabolism involving oxygen and electron transfer [1]. However, free heme is a potent pro-oxidant that catalyzes the generation of reactive oxygen species (ROS) leading to cellular damage [2]. Heme oxygenas
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