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Theoretically the majority of resistance mechanisms identifi
2022-08-19

Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei
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In our previous study we designed
2022-08-19

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic Memantine hydrochloride (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in
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Reduction of the hydrolysis of ATP
2022-08-19

Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct
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In this study we demonstrate that HHcy
2022-08-19

In this study, we demonstrate that HHcy upregulated the expression of GSNOR in T cells. As a result, GSNOR induced denitrosylation of Akt in Hcy-activated T FPH2 in vivo and in vitro, which contributed to vascular inflammation and susceptibility to atherosclerosis in GSNOR-/-ApoE-/- mice. The transl
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Tankyrase Inhibitors 22 The Bcl and Bcl xL genes contain the
2022-08-19

The Bcl-2 and Bcl-xL genes contain the CRE binding site in their promoter regions for CREB and CBP to bind to, so CREB phosphorylation was shown to up-regulate these anti-apoptotic genes, Bcl-2 and Bcl-xL [[29], [30], [31]]. Bcl-2 and Bcl-xL prevent the activation of caspases and the release of mito
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protease activated receptor In this present study the availa
2022-08-18

In this present study, the availability of commercial GLUT and SGLT protease activated receptor directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these re
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High lipophilicity of seems to
2022-08-18

High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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br Introduction The term autophagy
2022-08-18

Introduction The term “autophagy” was coined by Christian de Duve in 1963 to describe the process of removing and degrading intracellular components such as unused proteins and damaged organelles through lysosomes [1,2]. Autophagy has been divided into three main types, namely, macroautophagy, mi
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Importantly both genetic deletion and pharmacological inhibi
2022-08-18

Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the
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To date the crystal structures of
2022-08-18

To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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In this study we evaluated and compared the kinetics and
2022-08-18

In this study we evaluated and compared the kinetics and duration of the oral and systemic HPV-16 and HPV-18 specific antibody response to three doses of the qHPV vaccine in mid-adult aged HIV+ men from the AIDS Malignancy Cohort (AMC) 052 trial and mid-adult aged HIV− men from the Mid-Adult Male [M
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Tanshinone IIA It is important to highlight that glucose dep
2022-08-17

It is important to highlight that glucose-dependent generation of OMP of high magnitudes occurs due to the voltage-gating properties of VDACs, because only small magnitudes of OMP were obtained when the VDAC voltage sensitivity was zero (Fig. 5). These results indicate a possible physiological role
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Long term effects of prolonged darkness
2022-08-17

Long-term effects of prolonged darkness on specific physiological activities were also monitored at different leaf positions. Basically, stomatal conductance and CO2 assimilation were different at various leaf stages and were decreased or inhibited significantly within 24 h in all leaf positions upo
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Recently it has been found that treatment of
2022-08-17

Recently, it has been found that treatment of human phagocytic Vinorelbine or microvascular endothelial cells with NO donors inhibited the O2− generating capacity of NADPH oxidase [[8], [9], [10], [11]], which may involve down-regulation or S‑nitrosylation of the p47phox subunit (a cytosolic subuni
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The frequency of GSTM and GSTT null
2022-08-17

The frequency of GSTM1 and GSTT1 null genotypes vary in different populations. For example, Hiragi et al. (2007) reported a frequency of 17–35% for the GSTM1 null genotype and 22–44% for the GSTT1 null genotype in Brazilians of African descent (Hiragi et al., 2007). Chen, Liu, and Relling (1996) rep
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