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BMN-673 australia Tacrine an aminoacridine derivative Fig A
2022-12-15
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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br Acknowledgements MC and PD
2022-12-15
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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From our in vivo studies and previously reported
2022-12-15
From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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The activity of an enzyme may be regulated allosterically
2022-12-15
The activity of an enzyme may be regulated allosterically as well as transcriptionally. We have consistently studied REMS deprivation (REMSD) associated NA mediated allosteric regulation of Na-K ATPase activity in neurons and glia in vivo and in vitro (Amar and Mallick, 2015; Amar et al., 2016; Bask
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br Results br Discussion Control of chronic inflammation is
2022-12-14
Results Discussion Control of chronic inflammation is important in several inflammatory conditions like asthma, rheumatoid arthritis and fibrosis in lung diseases. The regulatory pathways that control chronic inflammation are complex and multi-factorial. Over expression of inflammatory mediat
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br Future directions outlook Peptide based macrocycles are a
2022-12-14
Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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br Funding This study was supported by a grant from
2022-12-14
Funding This study was supported by a grant from the Science and Technology Program of Guangzhou (No. 2014Y2-00181) and the personnel training program of Southern Medical University (No. PY2015N023). Conflict of interest statement Authors’contributions Introduction Chronic cerebral hypo
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br Conflict of interest statement br
2022-12-14
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse phar
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The first identified auxiliary subunit stargazin is essentia
2022-12-14
The first identified auxiliary subunit, stargazin, is essential for AMPAR function in cerebellar granule neurons (Hashimoto et al., 1999). Subsequently, a family of six transmembrane AMPAR regulatory proteins (TARPs) were defined that modify channel trafficking, gating, and pharmacology (Kato and Br
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Considering our previous results with cfDNA in EGFR TKI
2022-12-14
Considering our previous results with cfDNA in EGFR TKI-resistant NSCLC patients and growing evidence about different mutations in the ALK kinase domain as responsible for acquired resistance to ALK TKIs, we planned this study. Even if a next-generation sequencing approach after PD during crizotini
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In large biopsies series from ALK NSCLC treated patients the
2022-12-14
In large biopsies series from ALK+ NSCLC treated patients, the number of detected mutations increased after second generation ALKi (Gainor et al., 2016) and in one study were present in 56% of the entire cohort (Shaw et al., 2013b). For example, the rate of G1202R mutations increases from 2% in post
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Acetaminophen N acetyl p aminophenol AAP Fig
2022-12-14
Acetaminophen (N-acetyl-p-aminophenol, AAP) (Fig. 1) is a medically important, low cost, readily available and commonly used over the counter analgesic and antipyretic drug [18,19]. Acetaminophen monotherapy is efficient and is safer than Aspirin and Ibuprofen [20]. The efficacy and tolerability in
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AKT activity is also self limiting through its substrate
2022-12-14
AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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br Experimental procedure br Introduction Migraine is a debi
2022-12-13
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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All scientific data over the years points that reductase inh
2022-12-13
All scientific data over the years points that 5α-reductase inhibitors undoubtedly are an effective treatment for BPH and associated LUTS, having a favorable risk-benefit profile. In contrast, although some studies indicated positive results, there is still no consensus about their use in BPH or PC
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