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High throughput screening HTS of the AstraZeneca compound co
2020-12-25

High throughput screening (HTS) of the AstraZeneca fluvastatin sale collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) an
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Saito et al reported that d http
2020-12-25

Saito et al. reported that diabetic bone has lower lysyl oxidase-derived enzymatic cross-links in collagen compared to non-diabetic bone, based on studies performed in a rat model [9]. Lysyl oxidase plays a pivotal role in bone development and function, as revealed in classical studies [10], [11]. L
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The lungs dissected from week mice were cut into small
2020-12-25

The lungs dissected from 4–5-week mice were cut into small pieces and then immersed in Dulbecco's modified Eagle's medium (Invitrogen, Carlsbad, CA) containing collagenase II (2 mg/ml), trypsin (2.5 mg/ml), Dnase I (2 mg/ml), penicillin (100 U/ml), and streptomycin (100 μg/ml) for 12 hours at 37 °C
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Gemcitabine Our finding that activating DDR variants are a
2020-12-25

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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br Conclusion br Funding source br Ethical
2020-12-25

Conclusion Funding source Ethical approval Conflict of interest statement Introduction Traditionally, schizophrenia (SZ) was thought to be associated with neuronal dysfunction; however, the current hypothesis that myelin and, specifically, oligodendrocytes are also involved in the dev
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Given the importance of cysteine cathepsin inhibitors as
2020-12-25

Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Introduction The Bromeliaceae family is one of the
2020-12-25

Introduction The Bromeliaceae family is one of the most morphologically and ecologically diverse flowering plant families native to the tropics and subtropics of the New World (Benzing, 2000). They comprise >3000 species and are traditionally divided into three subfamilies: Pitcairnioideae, Bromeli
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br Role of cysLT signaling on various neurological
2020-12-25

Role of cysLT signaling on various neurological complications which are associated with Alzheimer’s disease Alzheimer’s disease, first described in 1906 by Alois Alzheimer, is a neurodegenerative disease and a very common cause of dementia progressively leading to death. Even though years of rese
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Although several examples of selective reduction of
2020-12-25

Although several examples of selective Biperiden HCl mg of α-diazoesters to α-hydrazonoesters have been described in the literature, reports on practical and general examples of such a process are scarce. In this context, there was a need to devise a mild and general method for the selective reduct
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The CYP A genes are
2020-12-25

The CYP3A genes are regulated physiologically by glucocorticosteroids, growth hormone, thyroid hormones and cytokines [13, 20, 30]. It has been shown that glucocorticoid receptor (GR), pregnane X receptor (PXR), constitutive androstane receptor (CAR) and vitamin D receptor (VDR) play an important ro
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The requisite extended benzyl alcohols
2020-12-25

The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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br Nuclear export and the functions of
2020-12-25

Nuclear export and the functions of CRM1 The nuclear envelope provides a compartmentalized intracellular environment for DNA replication, the synthesis of RNA, and production of ribosomes, and, as such, it can regulate cellular biological processes including apoptosis and proliferation. Nucleocyt
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br Methods br Results Our study
2020-12-24

Methods Results Our study focused on consecutive postural adjustments (CPAs) between IS and BS (the shaded areas on Fig. 2); that is to say, the Rx kinetics that occur after the end of an upper limb movement. It was dedicated to examining the main features of CPAs and the influence of movement
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Tinnitus Met carriers with severe hearing loss perceive
2020-12-24

Tinnitus Met carriers with severe hearing loss perceive their tinnitus as being louder, which is associated with increased activity in the PHC, increased PHC→pgACC connectivity, as well as decreased pgACC→PHC connectivity. This indicates that Met carriers with severe hearing loss have increased tinn
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Grapiprant is a selective antagonist for prostaglandin E PGE
2020-12-24

Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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