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A high throughput screening campaign led to the discovery of
2023-09-07
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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However in recent years advanced experiments and findings
2023-09-07
However, in recent years advanced experiments and findings are emerging to give us more detailed information on Aβ-membrane interactions. Several reviews have provided background on the fibrillation of Aβ and the Aβ-membrane interactions [[18], [19], [20], [21], [22]]. In this review, we mainly focu
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ARRY-380 LAP locations in the parasite tissues would
2023-09-07
LAP locations in the parasite tissues would provide clues for the potential physiological roles of it inside the parasite body. To date, tissue localization of LAPs has been carried out in many helminth parasites; however, information regarding LAPs in tapeworm is scarce. It was shown that LAPs were
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br Impact of global AHR deficiency on diet induced
2023-09-07
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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br Funding This work was
2023-09-07
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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TMP269 mg Further evidence for ACh GABA cotransmission had a
2023-09-07
Further evidence for ACh/GABA cotransmission had also been observed in the cortex. Extensive axonal arborization from cholinergic BF neurons exists throughout the cortical layers, allowing direct observation of cholinergic synaptic terminals. One study in the visual cortex of cat examined immunolabe
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Bioactive peptides contain amino acids
2023-09-07
Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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Molecular docking is widely used to predict the
2023-09-07
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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Introduction The lysosomal storage disorder
2023-09-07
Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat
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The srd a isoforms showed
2023-09-07
The srd5a isoforms showed unique expression profiles in early FHM development (Fig. 2). Similar to amphibian embryos, there was a high abundance of both srd5a1 and srd5a3 at 1dpf in FHMs, suggesting that mRNA for these enzymes may be maternally deposited and that these enzymes may play a key role in
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For both the hydroxylation and lyase reactions the heme iron
2023-09-07
For both, the 17α-hydroxylation and 17, 20-lyase reactions, the heme iron center of P450 17A1 receives electron reducing equivalents from CPR. Both reactions require one pair of electrons and molecular oxygen for the conversion of the substrate into product in each catalytic cycle. However, the 17,2
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The analysis of the profile of protein phosphorylation in MM
2023-09-06
The analysis of the profile of protein phosphorylation in MMS-treated R-848 confirmed that both the ATM and ATR pathways were activated in S-phase blocked cells. Interestingly, phosphorylation of Chk1 was observed 24h after MMS-treatment both in AT- and ATM-inhibited cells, whilst in the absence of
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Aromatization of the pyrrole ring after
2023-09-06
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Cerebral ischemia occurs following the occlusion of
2023-09-06
Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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br The role of apelin in hypertension diseases The
2023-09-06
The role of apelin in hypertension diseases The role of apelin and its receptor APJ in cardiovascular diseases has been described in numerous studies (Table 2) [36,37]. It has been revealed that exogenous apelin may lower blood pressure. Tatemoto et al. [6] have discovered that different forms of
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