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In earlier experiments on snails a behavioral model was empl
2023-07-19
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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AZ191 While A Rs communicate mainly with the D R
2023-07-19
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this AZ191 area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. This interac
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A high throughput small molecule ACK
2023-07-19
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found (3S,5S)-Atorvastatin sodium salt to be both ATP-competitive and reversible. Early structure-activity relationsh
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br In patients with spina bifida and spinal cord injury
2023-07-19
In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all
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Introduction Chronic inflammation is increasingly known
2023-07-19
Introduction Chronic inflammation is increasingly known as one of the most critical etiological factors in gastrointestinal (GI) cancers (Lee et al., 2016; Wang and Cho, 2015). Overexpression of 5-lipoxygenase (5-LOX), 5-LOX-activating protein (FLAP), as well as other leukotriene (LT) biosynthetic
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In young animals the HT A receptor antagonist ketanserin
2023-07-19
In young animals, the 5-HT2A mitotic inhibitors antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots for th
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Several dehidropregnenolone derivatives functionalized at C
2023-07-19
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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Drug resistance development often involves
2023-07-19
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 pramiracetam are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associat
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NOXA a BH only protein is
2023-07-19
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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Previous studies have demonstrated that the expression
2023-07-19
Previous studies have demonstrated that the expression of the Aurora B gene is maximally increased at G2/M phage during mitosis (Honda et al., 2003, Fu et al., 2007, Goldenson and Crispino, 2015), and exhibits an extraordinary upregulation in a number of human cancers (Fu et al., 2007, Kollareddy et
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We wanted to investigate the influence of substituents on th
2023-07-19
We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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As shown in B the recombinant human LOX
2023-07-19
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic plicamycin and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disappear
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br Introduction In the past
2023-07-19
Introduction In the past two decades, graphene and graphene based nanomaterials with unique physicochemical properties have attracted great attentions in many fields including biomedicine and biotechnology. Graphene oxide (GO) and its derivatives have shown promising potential as biological and c
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There are however concerns of potential side effects
2023-07-19
There are however, concerns of potential side-effects that should also be taken into account. Even though some studies pointed towards a potentially greater radiosensitising effect in p53-deficient tumours, ATM inhibition radiosensitises Latrunculin B in general, which raises the concern of normal
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Most of lipid lowering agents have many therapeutic
2023-07-19
Most of lipid-lowering agents have many therapeutic problems with severe side effects, while dietary fibers as lipid lowering therapy are safer. Chitosan (CS) is a dietary fiber biodegradable, biocompatible and has many health benefits including wound healing, antiinflammatory, anti-cancers, immune-
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