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Based on the above we hypothesized that a PROTAC
2020-06-01
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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The reference standards methyl difluoro dioxolo benzo
2020-06-01
The reference standards methyl 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)carbamoyl)benzoate () and -(2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)-3-methoxybenzamide (), and their corresponding desmethylated precursors 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:
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In contrast to SQLE HMGCR could be efficiently degraded
2020-05-29
In contrast to SQLE, HMGCR could be efficiently degraded in Mepivacaine HCl lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our re
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The other scenario pertaining to the significance of
2020-05-29
The other scenario pertaining to the significance of H2AX phosphorylation is based on the fact that the initiation of DNA fragmentation by CAD facilitates the chromatin condensation that occurs concurrently [15]. Apoptotic DNA fragmentation and chromatin condensation are important for the efficient
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Cyclin D inhibits the transcriptional activity
2020-05-29
Cyclin D1 inhibits the transcriptional activity of the transcription factors myogenin and MEF2 [39,40]. In addition, myogenin activates MEF2 expression, which feeds back to amplify the myogenin promoter [38]. In this study, DGKδ suppression, in addition to the increase of cyclin D1, inhibited myogen
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DGK is also involved in
2020-05-29
DGKδ is also involved in cell differentiation. Previously, to investigate the physiological roles of DGKδ, DGKδ-deficient mice have been generated. On the basis of the analysis of DGKδ-deficient mice, Crotty et al. reported that DGKδ regulates the epidermal growth factor receptor (EGFR) pathway by a
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The data from drug screening
2020-05-29
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Predictions of enzyme topology for DGAT are more difficult
2020-05-29
Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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Industrial fermentation aims to produce valuable
2020-05-29
Industrial fermentation aims to produce valuable products from cheap feedstocks by utilizing diverse microbial functions through aerobic or anaerobic fermentation [[8], [9], [10]]. During anaerobic fermentation, the reducing power is mostly directed to product synthesis rather than being oxidized, r
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Various domains of DDR have been shown
2020-05-29
Various domains of DDR1 have been shown to be important for receptor clustering and its oligomeric status. It is now understood that (i) dimerization [7] and higher-order oligomerization [12], [18] of the DDR1 extracellular domain (ECD) enhance its binding to collagen; (ii) DDR1 exists as non-covale
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br Introduction Natural killer NK cells have an unique
2020-05-29
Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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LY2228820 The androgen receptor AR is a
2020-05-29
The androgen receptor (AR) is a steroid hormone receptor that plays a crucial role in the normal development of male reproductive tissues, and its high expression and/or relaxation of its regulation are strongly implicated in prostate cancer (PCa) [11]. Androgen binding induces conformational change
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Introduction Globally lung cancer has the
2020-05-29
Introduction Globally, lung cancer has the highest morbidity and mortality rates of all types of cancer, with 1.5 million patients newly diagnosed annually [1]. Approximately 85% of lung cancer cases are non-small cell lung cancer (NSCLC) [2]. The first-line treatment for NSCLC is surgical resectio
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br Results br Discussion Unraveling the molecular details
2020-05-29
Results Discussion Unraveling the molecular details of nucleoporin-karyopherin interactions, which have to be strong enough to promote transport but sufficiently weak to avoid stalling of transport complexes within the pore, is key to our understanding of the mechanisms of nucleocytoplasmic tr
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The proposed FDIR technique is presented in the following fo
2020-05-29
The proposed FDIR technique is presented in the following format: Section 2 contains a survey of typical orbits of interest with regard to the Cy7 NHS ester (non-sulfonated) environment found in them, which is contrasted with a LEO orbit. Additionally, how the requirements for the satellite system c
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