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The NF B family of transcription factors is involved
2022-01-13

The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) atp citrate lyase inhibitor against cadmium-induced oxidat
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Tamoxifen is still the most frequently
2022-01-13

Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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HOBt Functional studies based on patch clamp electrophysiolo
2022-01-13

Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single HOBt in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open state and
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Kern et al observed an overall improvement in behaviors typi
2022-01-13

Kern et al observed an overall improvement in behaviors typical for autism during TR. They used the Childhood Autism Rating Score (CARS), to determine the intensity of the change and found lower CARS values after 3 (t(21) = 2.73, p Fmoc-Asp(OtBu)-OH comparison of differences in QoL improvement in bo
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β-Sitosterol It is well known that GPCR responsiveness desen
2022-01-13

It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling
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Dioscin receptor Tail group SAR of the imidazole derived
2022-01-13

Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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Tetrazole is one of the most commonly used bioisosteres for
2022-01-13

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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br Introduction As is now well
2022-01-13

Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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Injury to oligodendrocyte progenitors caused in part by glut
2022-01-13

Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the
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With rare exceptions the biological role of secretase
2022-01-12

With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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br Introduction Thrombosis is one of the leading causes
2022-01-12

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable Phosphoramidon Disodium Salt and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts abo
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The electroconductive or electrocatalytic properties of cond
2022-01-12

The electroconductive or electrocatalytic properties of conductive moieties including polymers in combination with carbon or metal-based nanomaterials have also been explored. For example, Dong et al. (2017) developed a portable electrochemical immunosensor by creating a film of Prussian blue chitos
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Importantly recent in vivo results demonstrated
2022-01-12

Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla
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Suz is required for methyltransferase activity
2022-01-12

Suz12 is required for methyltransferase activity, silencing function, and PRC2 protein stabilization in somatic and human ESCs (Cao and Zhang, 2004, Pasini et al., 2004, Collinson et al., 2016). Our experiments indicate that, in addition to associating with the H3K27 demethylases KDM6A (UTX) (Wang e
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Initial experiments confirmed that RBC
2022-01-12

Initial experiments confirmed that RBC8 effectively inhibited both RalA and RalB activation in an identical, dose-dependent manner following platelet stimulation with the GPVI-specific ligand, CRP (Fig. 1Ai). Non-specific, upper bands were observed when immunoblotting for activated RalB, with the sp
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