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Encouraged by this observation a systematic
2024-07-05
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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rt pcr Herein we disclose novel dihydropyrano c pyrazoles th
2024-07-05
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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In the current study we provide evidence that
2024-07-05
In the current study, we provide evidence that enhanced ATX activity correlates well with increased ATX protein concentration during cholestasis and pregnancy (Fig. 1). Hereby we have ruled out the possibility of ATX enzyme activation in these conditions, e.g. by circulating cholephiles. ATX clearan
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Fucoidan br AMPK as a druggable target AMPK signaling has
2024-07-04
AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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Dose Response Studies Against Puromycin Sensitive Aminopepti
2024-07-04
Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino FTY720 Phosphate mg sequence, it has a broad substrate specificity, and is
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In brief serotonin can interact with
2024-07-04
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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Based on the improved characteristics of
2024-07-04
Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun
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In an insightful essay Heryanto writes that language
2024-07-04
In an insightful essay, Heryanto (1990, 40) writes that language is “a phenomenon expressing the particular history of a society” that did not exist in many parts of the world. “Language is not a universal category or cultural activity. Though it may sound odd, not all people have a language in the
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br Results br Discussion Dopamine regulates behavioral respo
2024-07-04
Results Discussion Dopamine regulates behavioral responses to nicotine in Drosophila (Bainton et al., 2000), but neurochemical measurements of dopamine after nicotine stimulation had not been made. Here, we demonstrate for the first time that the stimulation of nAChRs causes dopamine release i
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br Funding br Introduction l Dihydroxyphenylalanine l
2024-07-04
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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A contribution of V ATPase subunits specifically to
2024-07-03
A contribution of V-ATPase subunits specifically to phagosome-lysosome fusion was uncovered by Peri and Nüsslein-Volhard who described that depletion of the VO subunit a1 in zebrafish interferes with phagosome maturation in microglial Zinc protoporphyrin IX (Peri and Nusslein-Volhard, 2008). Howeve
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br Materials and Methods br Results br Discussion XHP is
2024-07-03
Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer Octyl-α-ketoglutarate in vitro, including Hs578T, MCF-7,
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Calmidazolium chloride Available data thus indicate that the
2024-07-03
Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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ACET These experiments make it clear that one
2024-07-03
These experiments make it clear that one can study the effect of antimalaria drugs that target the DHFR enzyme of P. falciparum by transferring the malaria enzyme into S. cerevisiae. The ease of growth and manipulation of the yeast make it easy to measure the sensitivity of any particular dhfr allel
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AG957 br Experimental procedures br Results br
2024-07-03
Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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