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IC values were obtained for
2024-07-24
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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In addition to drawing attention to Ser of
2024-07-24
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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From an historical perspective ligands for GPCRs adrenaline
2024-07-24
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, AZ3146 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were rap
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NU 9056 Most human diseases e g cancer diabetes and
2024-07-23
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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In a missense mutation at codon of
2024-07-23
In 1989, a missense mutation at codon 102 of the PRNP gene was first reported to be associated with GSS and, in 1991, the same mutation was also found in affected members of the “H” family (Hsiao et al., 1989; Kretzschmar et al., 1991). By 1995, the pedigree of the “H” family included 221 family mem
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5224 Elevated aminopeptidase activities were often detected
2024-07-23
Elevated aminopeptidase activities were often detected in organs of plant with accelerated protein turnover, such as leaves and petals during senescence, fruits maturation or in germinating seeds [22]. Moreover, it was proven that these enzymes take part in defense responses [[23], [24], [25]]. Part
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The synthetic route to M developed by Rice was
2024-07-23
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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A c and CD are expressed in a small
2024-07-23
A2c and CD73 are expressed in a small population of OSNs with pear-shaped morphology. In spite of the expression of molecular markers of ciliated OSNs such as Golf, ACIII, and OMP [1, 17], these OSNs have an extremely short dendrite and are located in the superficial layer of OE. In addition to the
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In this study we obtained the absorbance and
2024-07-23
In this study, we obtained the absorbance and photoluminescence (PL) of ZSTK474 australia polymerized with various types of actin-binding proteins in order to probe the actin structures in situ without labeling. Both optical measurements have been useful in examining biomaterials such as DNA and pro
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Busulfan The altered frequency of CD T
2024-07-23
The altered frequency of CD4+ T Busulfan in 5-LO−/− mice led us to hypothesize that these leukocytes could be exerting a primary control of the inflammatory response. In fact, the lack of 5-LO resulted in the accumulation of CD4+CD25+ cells expressing Treg markers. It is plausible to speculate that
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This study does have several limitations mainly related to t
2024-07-23
This study does have several limitations, mainly related to the DMSO vehicle. While DMSO is a known anti-inflammatory mediator,5, 12 it has been shown to upregulate ALOX5, which was not seen in this study (as we are likely underpowered to detect this difference). A manifestation of this anti-inflamm
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The obtained results indicate that even when the impairment
2024-07-23
The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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Here we show that the co activation of RTKs and
2024-07-22
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC NLG-8189 and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005 (
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Five alternatively spliced isoforms of ATX
2024-07-22
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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The earliest appearance of tumors
2024-07-22
The earliest appearance of tumors occurred at 12 months and the latest at 24 months, with an average onset at 18 months (Fig. 1B). This would be roughly equivalent to cancer presenting in a patient between 60 and 70 years of age. In transgenic animals, autotaxin Calyculin A was relatively increased
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