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Interest in natural products has led to the study
2024-08-30

Interest in natural products has led to the study of plant extracts as sources of ARIs. However, chemical complexity of natural extracts makes the identification of ARIs challenging and time-consuming. Identification of bioactive compounds with the desired biological effect from natural products, co
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br Acknowledgements This work was
2024-08-30

Acknowledgements This work was supported by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do Estado do Rio Grande do Sul (FAPERGS) FINEP research grant “Rede Instituto Brasil
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As a continuation of our search for a selective AChE
2024-08-30

As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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Very recently Niessen et al have described
2024-08-30

Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underline
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br Aurora A Aurora B and Aurora C small
2024-08-30

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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Song et al reported series of triazolylsalicylamide derivati
2024-08-30

Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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The uterine muscle also changes to meet the demands
2024-08-29

The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind
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Apelin APJ triggers a variety of cellular signaling pathways
2024-08-29

Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 s
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Autocrine regulations of several adipokines e
2024-08-29

Autocrine regulations of several adipokines (e.g., leptin and resistin) on adipocytes have been reported (Karastergiou and Mohamed-Ali, 2010, Ye et al., 2010). Several lines of evidence have shown that apelin influences adipocyte functions, such as, lipolysis and glucose uptake (Dray et al., 2008, Y
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In order to further explore whether the cytoprotective effec
2024-08-29

In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 pim inhibitor is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large
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br Genetic analysis of polarity complexes Model organisms su
2024-08-29

Genetic analysis of polarity complexes Model organisms such as Caenorhabditis elegans and Drosophila melanogaster provide useful means of describing basic biological processes. They lend themselves particularly well to addressing some of the questions arising in this field because of their struct
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Long term blood pressure regulation is linked to
2024-08-29

Long term blood pressure regulation is linked to renal function through the mechanisms of pressure natriuresis (Evans et al., 2005), which has been shown to be modulated by the RAS (Hall et al., 1999). Key components of the RAS are expressed throughout the kidney, and are implicated in renal excreto
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Perhaps the first evidence of AMPKs therapeutic ability
2024-08-29

Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle HC 067047 synthesis treated with MET, an AMPK activator and first-line therapy for type 2 diabetes me
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It has been reported that
2024-08-29

It has been reported that NLRP3 product, caspase-1, is increased in the brains of AD patients and experimental AD animals. NLRP3- and caspase-1-deficient animals are resistant to experimental development of AD, and have decreased IL-1β production and significantly increased Aβ clearance (Heneka et a
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Sweroside br Introduction Diabetes mellitus DM is a chronic
2024-08-29

Introduction Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated levels of glucose in the blood. Type 1 diabetes is characterized by insufficient insulin production and needs a daily administration of insulin. Actually, no prevention is known for Type 1 diabetes. Type
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