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Finally considering the encouraging inhibitory and selectivi
2021-06-07

Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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Besides the assessment of toxicological effects immediately
2021-06-07

Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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In rodents but not humans
2021-06-07

In rodents but not humans, two splice variants of Chk are identified as Ntk and Ctk, which possess and lack the N-terminal unique domain, respectively. While Ctk is abundantly expressed in the brain, Ntk is selectively restricted to myeloid and lymphoid cells, especially megakaryocytes [31]. This ra
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Introduction Taenia solium is the causative agent of
2021-06-05

Introduction Taenia solium is the causative agent of human taeniasis/cysticercosis and porcine cysticercosis, a major health problem and a veterinary economic challenge in developing countries of Latin America, Africa, and Asia. In Mexico, approximately 500 human neurocysticercosis cases were repor
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Our results demonstrated that ET a Wnt ligand stimulated the
2021-06-05

Our results demonstrated that ET-1, a Wnt ligand, stimulated the Wnt/β-catenin signaling pathway. First, ET-1/ETRA binds to Frizzled family cell-surface receptors, resulting in the activation of Dvl1, a Dishevelled (DSH) family protein. Next, activated DSH inhibits the Axin, GSK-3β, and APC protein
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br Conflict of interest br
2021-06-05

Conflict of interest Introduction Endothelin receptors are members of the superfamily of G-protein-coupled receptors (GPCRs) and central regulators of vascular tension and other physiological functions in higher eukaryotes [1]. The human endothelin system comprises the highly homologous endoth
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Multiple protein species are known to naturally exist
2021-06-05

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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br Significance Our understanding of the ubiquitin
2021-06-05

Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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Immunofluorescence assays were performed to localize the enz
2021-06-05

Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the Escitalopram Oxalate generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with ant
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The ribosomal synthesis of D proteins is not currently
2021-06-05

The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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The compounds were ranked based on the Glide XP Score
2021-06-05

The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR a
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High throughput screening HTS of the AstraZeneca
2021-06-05

High throughput screening (HTS) of the AstraZeneca Chlorhexidine digluconate australia collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inh
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Overall the DDR kinase domain has a typical kinase
2021-06-05

Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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There was a measurable worsening but not a statistically sig
2021-06-04

There was a measurable worsening, but not a statistically significant change in the baseline and follow-up best ear hearing scores, where the mean worsening change was 11.9 dB (95% CI: −1.11–24.86, p-value = 0.070). However, of the 16 patients, 14 (87.5%) were found to have clinically significant wo
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br Introduction Al Awqati and his colleagues
2021-06-04

Introduction Al Awqati and his colleagues using R(+)-methylindazone, R(+)-[(6,7-dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy] acetic rusty (IAA-94) (Landry et al., 1987) isolated the first chloride intracellular ion channel (CLIC) proteins (p64) from bovine kidney cortex
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