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The first rationally designed dual mPGES LO inhibitor was
2023-02-20
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic A 61603 hydrobromide australia - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivativ
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br Funding This work was supported by Arena Pharmaceuticals
2023-02-20
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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Based on the observation that antipsychotic drugs
2023-02-20
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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Several approved and or experimental drugs
2023-02-20
Several approved and/or experimental drugs, together with natural compounds, have been reported to induce autophagy in different cancer types [70], [71], [72] (Table 1). In the next paragraphs, we will review more in detail a group of these agents selected in relation to their promising future outco
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GABAB receptor is associated with brain
2023-02-20
GABAB receptor is associated with EMD638683 sale and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in pa
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br Experimental section br Acknowledgments br Introduction A
2023-02-20
Experimental section Acknowledgments Introduction Adipose is a major endocrine organ which releases a range of bioactive agents [1]. Selected adipose depots have been established as sites of sex steroid metabolism [1]. Subcutaneous and visceral adipose express high levels of aromatase, cap
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Introduction Preeclampsia a serious hypertensive disorder
2023-02-20
Introduction Preeclampsia, a serious hypertensive disorder that can occur during pregnancy, is a pregnancy-related disease characterized by the onset of PRIMA-1 sale and proteinuria after the 20 t h week of gestation, and it occurs in about 5% of all pregnancies [1]. If left untreated, preeclampsia
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br Results br Discussion Control of chronic inflammation is
2023-02-20
Results Discussion Control of chronic inflammation is important in several inflammatory conditions like asthma, rheumatoid arthritis and fibrosis in lung diseases. The regulatory pathways that control chronic inflammation are complex and multi-factorial. Over expression of inflammatory mediato
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Finally we argue that the estimated penetrance of CI
2023-02-20
Finally, we argue that the estimated penetrance of 0.45% (95% CI 0.02%, 9.35%) calculated by leveraging the gnomAD (Lek et al., 2016) population data indicate that T201S is at most a low-risk gene variant for CJD. If we arbitrarily consider a central estimate of 10% or higher as the clinically signi
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br Mechanism of action In
2023-02-20
Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra
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br Materials and methods br Results br Discussion We
2023-02-20
Materials and methods Results Discussion We demonstrate reduced angiogenic activity in NDRG1 overexpressing malignant glioma leading to reduced glioma growth. This antiangiogenic phenotype is paralleled by a significant upregulation of the antiangiogenic gene TNFSF15. TNFSF15 upregulation i
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APP is a member of a
2023-02-20
APP is a member of a conserved protein family that also includes amyloid precursor-like proteins 1 and 2 (APLP1, APLP2).8, 9, 10 The proteins in this family are type I single-pass transmembrane 1632 with receptor-like structural features but not entirely clear cellular functions.11, 12, 13, 14 Thes
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br Results br Discussion Here we uncovered a role
2023-02-20
Results Discussion Here, we uncovered a role for Wnt-Fz7 signaling in LTP-dependent spine plasticity and synaptic localization of AMPARs. We demonstrated that LTP induction increased Wnt7a/b protein at Doxycycline HCl and spines. Direct blockade of endogenous Wnts impaired LTP-mediated structu
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Analysis of the crystal structures
2023-02-20
Analysis of the crystal structures of LAPs from E. coli[29], bovine eye lens [30], Pseudomonas putida[27], tomato [31] and P. falciparum[32] revealed that the monomer of M17-family LAP is composed of two domains: the smaller, variable N-terminal domain and the larger, conserved C-terminal domain tha
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These mutations induce the gene auto activation in of adenoc
2023-02-20
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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