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Introduction Mammalian cells express the seven STAT
2025-02-17

Introduction Mammalian Pyrazinecarboxamide derivative express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of k
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The purpose of the present study is to characterize AChE
2025-02-17

The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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Another open question is whether GABA and
2025-02-17

Another open question is whether GABA and ACh are released from the same synaptic vesicles, or even the same presynaptic terminals. Multi-transmitter neurons may either function through co-release, in which multiple neurotransmitters are packaged into the same presynaptic terminal and are therefore
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br Materials and methods br Results Bilateral microinjection
2025-02-17

Materials and methods Results Bilateral microinjections (n = 6) of 10 mM ACh (300–500 pmol) and 5 mM physostigmine (150–250 pmol) at the two selected caudal NTS sites caused within 1 min significant increases in respiratory frequency (from 54.5 ± 1.7 to 70.9 ± 4.1 breaths/min; +30.8 ± 7.0%; P
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There are several reports about the expression of AChRs
2025-02-17

There are several reports about the expression of AChRs and their modulation to osteogenic factors in osteoblasts (Rothem et al., 2011, Sato et al., 2010, Walker et al., 2001). The normal osteocytic MLO-Y4 Polybrene in viral infection expressed multiple subtypes, which was demonstrated by the detec
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It has been reported that leukotrienes and their receptors e
2025-02-17

It has been reported that leukotrienes and their receptors, e.g. the cysteinyl leukotriene receptor 1 (CysLT1) may promote NF-κB pathway inhibitors injury (Ding et al., 2007) and that increased 5-LOX expression and activity lead to production of brain-toxic molecules (Khan et al., 2010). However, di
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Introduction Chronic inflammation is increasingly known as o
2025-02-17

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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The synthesis and secretion of adrenal androgens is
2025-02-17

The synthesis and secretion of adrenal androgens is apparently unique to humans and nonhuman primates, and requires the expression of key mediators such as CYP17 [26]. Endocrine control of CYP17 expression in rhesus monkeys is comparable to that in humans [27]. An analysis of baboon cDNA for CYP17 s
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Here we show that the co activation of RTKs and
2025-02-17

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC jnk inhibitor and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-
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In our previous report we synthesized derivatives with some
2025-02-17

In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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Most human diseases e g cancer
2025-02-15

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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br Implementation of sacubitril valsartan into clinical prac
2025-02-15

Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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Intriguingly androgens may also have an indirect effect
2025-02-15

Intriguingly androgens may also have an indirect effect on AR gene expression through inhibition of the GATA2 transcription factor gene (He et al., 2014) (Table 1). Using ChIP-seq, GATA2 was found to bind to a regulatory element 5.5 kb upstream of the TSS of the AR gene and enhanced transcription, w
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Amyloid fibrils are insoluble high molecular
2025-02-15

Amyloid fibrils are insoluble, high-molecular-weight, non-crystalline aggregates and traditional experimental techniques for structure determination such as X-ray and solution NMR cannot resolve their high resolution structures [64], [68]. However, amyloid fibrils exhibit various advantageous featur
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Through an extensive SAR optimization campaign
2025-02-15

Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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