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br Dienogest DNG Dienogest is a
2020-07-06

Dienogest (DNG) Dienogest is a 19-nortestosterone derivative with two special structural changes [Fig. 1a]: [a] At the cabon-17 position there is a cyanomethyl group instead of an ethinyl group; [b] A double bond is present between carbons 9 and 10. DNG is the only progestogen that combines prope
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Raloxifene is a second generation SERM that has tissue
2020-07-06

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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PI K Akt signaling pathway
2020-07-06

PI3K/Akt signaling pathway is known in modulating cell apoptotic process (Saurus et al., 2015). To study the contribution of PI3K/Akt signaling pathway in ERRγ-mediated anti-apoptotic effect in podocytes, we examined phosphorylation of Akt and expression of PI3K subunits p110α and p85α via qRT-PCR a
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DDR expression is upregulated in the
2020-07-03

DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident Azithromycin is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favo
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bio bio We did not observe inhibition of vCPH
2020-07-03

We did not observe inhibition of vCPH by any of the TCA cycle intermediates (apart from the metal chelators citrate and isocitrate), nor by the factor inhibiting HIF (FIH; a 2OG-dependent asparaginyl hydroxylase) inhibitor N-oxalyl d-phenylalanine (NOF) or the γ-butyrobetaine dioxygenase inhibitor m
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In our previous research we have focused
2020-07-03

In our previous research, we have focused on the discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Numbers of biphenyl-aryl urea incorporated with salicylaldoxime including BPS-7 have been developed as potent and selective VEGFR-2 inhibitors (Fig. 3) [12], [13], [14], [15], [16], [1
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Conessine receptor Crystallographic and NMR based analyses h
2020-07-03

Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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Adrucil br Acknowledgments br Introduction Cysteinyl leukotr
2020-07-03

Acknowledgments Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic Adrucil and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3],
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br P Y receptor structure br Pharmacology Several subtype
2020-07-03

P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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br Results and discussion br Conclusion In
2020-07-03

Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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MAPKs are a family of phosphorylating enzymes that
2020-07-03

MAPKs are a family of phosphorylating enzymes that orchestrate various cellular response in proliferation, apoptosis, inflammation, stress response, and energy metabolism [11]. There are at least four major members including extracellular signal-regulated kinase 1 and 2 (ERK1/2), p38 mitogen-activat
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br Acknowledgments The authors thank
2020-07-02

Acknowledgments The authors thank Elisabete Lepera and Rosana Silva for technical support. The study was supported by FAPESP, CNPq and PADC/FCF-UNESP. T.T. Miguel was the recipient of a FAPESP (Proc. 05/05171-1) and R.L. Nunes-de-Souza of a CNPq (Proc. 303580/2009-7) fellowship. Introduction
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There are two general approaches to building Bayesian
2020-07-02

There are two general approaches to building Bayesian networks for the purpose of risk assessment. Researchers can implement static models that predict risk or survival at a snap-shot of time. For example, Loghmanpour et al. [10] created Bayesian network-based risk assessment models for patient data
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br Introduction Epithelial mesenchymal transition
2020-07-02

Introduction Epithelial-mesenchymal transition (EMT) is a biological process by which epithelial 130 ml synthesis lose cell polarity and cell-cell adhesion, and gain mesenchymal features with an increase of migratory and invasive properties [1]. EMT is essential for mesoderm formation during emb
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In the present work we have investigated the reactivity of
2020-07-02

In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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