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To efficiently develop bioactive ligands even if
2022-08-16

To efficiently develop bioactive ligands even if the structural information of the target protein is unknown, we have presented a three-dimensional structural diversity-oriented strategy based on structural properties of a chiral cyclopropane. Our strategy has allowed us to design and synthesize a s
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Ro 31-8220 Mesylate br Methods br Acknowledgements We are gr
2022-08-16

Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo
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FoxM a downstream target of Gli
2022-08-16

FoxM1, a downstream target of Gli, has been mainly related to Compound C regulation and cellular proliferation in tumor (Alvarez-Fernandez and Medema, 2013, Halasi and Gartel, 2013, Teh et al., 2002). Especially, FoxM1 is a regulator of G1/S and G2/M transitions and M-phase progression (Wonsey & Fo
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NCSs are helical proteins containing four EF hand
2022-08-16

NCSs are α-helical proteins containing four EF-hand motifs with EF1 being incapable of Ca-binding throughout the family (atomic-resolution structure was firstly resolved for recoverin [5]; for review on NCS structure, see [6]). Some of the NCS proteins (i.e. recoverin and KChIP3) have two while othe
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Both anxiety like behavior and sucrose preference intake wer
2022-08-15

Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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br Materials and methods br Results Aberrant
2022-08-15

Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas
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br Central control of GI
2022-08-13

Central control of GI ghrelin secretion The CNS communicates with the GI tract through the vagus nerve originating in the DMV and sympathetic spinal afferents emanating from the thoracic spinal chord (Bray, 2000). The cells that secrete peripheral ghrelin are under direct control of these two pat
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GSIs were shown to effectively decrease A
2022-08-13

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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With the identification of small nonpolar
2022-08-13

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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Brain derived neurotrophic factor BDNF is the most abundant
2022-08-13

Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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Although pharmacological studies from the end
2022-08-13

Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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Andexanet alfa works as a decoy for the FXa inhibitor
2022-08-13

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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br Acknowledgment S A was supported by V
2022-08-13

Acknowledgment S.A was supported by V Plan Propio US-Acceso USE-14793-G. Introduction The Hippo signaling pathway is an evolutionarily conserved pathway that controls organ size and cell differentiation across diverse organisms through the regulation of cell proliferation and apoptosis (Di Ca
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In addition to lifestyle factors genetic factors may also in
2022-08-13

In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808
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Since we found miR b p to be differentially expressed
2022-08-12

Since we found miR-15b-5p to be differentially expressed along the porcine intestine in 31 day old piglets in a former study [10], the entire miRNA family was analyzed in terms of interaction with potential target-genes. In silico analysis predicted miR-15 family members to target the hedgehog signa
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