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GIPR genes were not found in any
2021-10-01

GIPR genes were not found in any of the available bird genome as well as the genomes of several species of fish (Tables S3 and S4). The genomic neighborhoods surrounding the GIPR genes in species that have them was generally conserved (see Fig. 8), and like GLP2R, those fish that did have a Gipr gen
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During the course of the development
2021-10-01

During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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In this review we will highlight how the functional
2021-10-01

In this review we will highlight how the functional impact of GABA receptors activation in thalamic neurons far exceeds the traditional “shunting” effect and shapes the whole thalamic network excitability. We will show how GABA released during either tonic or burst firing of GABAergic thalamic neuro
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A repertoire of cytotoxic payloads is
2021-09-30

A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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br Acknowledgements br Funding This work
2021-09-30

Acknowledgements Funding: This work was supported by the Instituto Nacional de Biomedicina do Semiárido (INCT-IBISAB-CNPq), Edital MCT/CNPq N° 014/2010 - Universal and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). Introduction Guanylin and uroguanylin are small, heat
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Cichlasoma dimerus as most teleost fish species present
2021-09-30

Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most NPS-2143 species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (González-
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In this study we provide biochemical and
2021-09-30

In this study we provide biochemical and immunohistochemical evidence for the localization of the glycine transporter GLYT1 in synaptic vesicles. Previously, it was thought that GLYT1 was exclusively a glial protein (Zafra et al., 1995a). However, due to a partial discrepancy between mRNA and protei
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The effects of these steroids namely the decrease
2021-09-30

The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the
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Both anxiety like behavior and sucrose preference
2021-09-30

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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In the present study five
2021-09-30

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Structurally the termini of FGF are critical for effective s
2021-09-29

Structurally, the termini of FGF21 are critical for effective signaling. Progressive amino nisin truncation at either end of the protein sequentially impairs FGF21 bioactivity, but via different mechanisms. Shortening at the N-terminus weakens its ability to activate the FGFR/KLB-complex but does n
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In the FARM motifs of GGPPSs hydrophobic amino
2021-09-29

In the FARM motifs of GGPPSs, hydrophobic Celecoxib are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP synthase (GGPPS)
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In order to estimate the influence
2021-09-29

In order to estimate the influence of mitochondrial hypo-polarization on generated OMP, IMP was changed from the normal value of Δψi = −140 mV (Fig. 4A, D, G) to Δψi = −100 mV (Fig. 4B, E, H), resulting in lower magnitudes of calculated OMP for hypo-polarized Tubacin (Fig. 4B). Similarly, a remarkab
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The site of metastasis in breast cancer
2021-09-29

The site of metastasis in breast cancer often contributes to the patient’s OS. Patients with bone metastasis from their breast cancer often have a notably increased survival over patients with visceral or hqn metastasis. In this analysis, ER+/HER2+ patients were noted to have a higher rate of bone m
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Starting from the hypothesis that the linker portion of
2021-09-29

Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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