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Inhibition of autophagy has been shown to alleviate neuronal
2023-09-01

Inhibition of autophagy has been shown to alleviate neuronal damage after cerebral ischemia, both in cell culture and rodent models (Koike et al., 2008, Li et al., 2015, Wang et al., 2016, Zhang et al., 2014, Zheng et al., 2014). Therefore, blockage of autophagy is a potential target for prevention
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Various compounds have been designed
2023-09-01

Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic citco sale moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a po
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Interestingly intermittent high doses of AKT inhibitors have
2023-09-01

Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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APPL is highly expressed in pancreatic cells but
2023-09-01

APPL1 is highly expressed in pancreatic β cells, but its levels are significantly decreased in several mouse models of obesity and diabetes, including HFD-induced obese mice and db/db mice [6], [73], suggesting that the dysregulation of APPL1 may be associated with malfunction of the pancreas in obe
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cddo Derivatives of M that possess either
2023-09-01

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these cddo to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrated to
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DMP 777 Since pyrrolopyrimidine dithiolanes and both display
2023-09-01

Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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PC is considered as a cancer of the epigenome Grasso
2023-09-01

PC is considered as a cancer of the epigenome (Grasso et al., 2012, Robinson et al., 2015). Our results demonstrate that the interaction of AR with ACK1 drives the positive feedback epigenetic circuitry that is ultimately conducive to promote AR transcription. Further, this circuitry subjugates AR t
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To maintain ATP levels postmortem muscle mobilizes
2023-08-31

To maintain ATP levels, postmortem muscle mobilizes its glycogen reserves to yield MAZ51 6-phsphate that proceeds through glycolysis. Glycogen degradation was affected by the interaction between treatment and time (P mitochondria had lower glycogen (P=0.05) than that of control, while samples contai
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Acl converts cytosolic citrate CoA and ATP into acetyl
2023-08-31

Acl converts cytosolic citrate, CoA and ATP into acetyl-CoA, ADP+Pi and oxaloacetate (Fig. 1). This cytosolic enzyme is present in few Prokaryotes and in all Eukaryotes, but not in non-oleaginous yeasts [14]. Thus, this enzyme was presumed to be essential for FA synthesis [1], [13], [15]. In most mi
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To evaluate the ability of both sets of compounds
2023-08-31

To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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The first objective of the present
2023-08-31

The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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Therefore a number of homoisoflavonoids
2023-08-31

Therefore, a number of homoisoflavonoids may be designed in future that may be effective against angiogenesis for treating ocular neovascularization. As this LB Broth, Miller current study deals with robust molecular modeling techniques on SH-11037 (cpd 15) and related homoisoflavonoids and SH-1103
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RNA interference assays have shown that the inhibition of AM
2023-08-31

RNA interference assays have shown that the inhibition of AMPK expression leads to increases in TNF-α, IL-6 and cyclooxygenase-2 (COX-2) levels after LPS stimulus, whereas the transfection of macrophages with a constitutively active form of AMPKα1 results in decreased LPS-induced TNF-α and IL-6 prod
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Enzalutamide Analysis of the crystal structures of LAPs from
2023-08-31

Analysis of the crystal structures of LAPs from E. coli[29], bovine eye lens [30], Pseudomonas putida[27], tomato [31] and P. falciparum[32] revealed that the monomer of M17-family LAP is composed of two domains: the smaller, variable N-terminal domain and the larger, conserved C-terminal domain tha
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Initially DPP DPP and prolyl tripeptidyl peptidase A
2023-08-31

Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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