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Collectively the results presented here provide new insights
2020-11-03

Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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br Chagas disease and HAT drug R D Drug R
2020-11-03

Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among
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RNA sequencing RNA seq is a particularly effective technolog
2020-11-03

RNA-sequencing (RNA-seq) is a particularly effective technology for gene discovery in a given process, especially in non-model species for which reference genome sequences are not available. Although the major application of RNA-seq analyses is the identification of differentially expressed genes (D
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Ethyl naphthoates a h were successfully reduced to naphthylm
2020-11-02

Ethyl 1-naphthoates (10a–h) were successfully reduced to 1-naphthylmethanols (12a–h) by using LiAlH4 with 8–87% yields. Then PCC was used to convert the alcohols into the corresponding 4-alkyl-1-naphthaldehyde derivatives (13a–h) with relatively higher yields (58–90%) as represented in Scheme 2. The
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The inhibition of mRFP Ub E formation by
2020-11-02

The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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The ability of minor groove binding agents to inhibit the
2020-11-02

The ability of minor groove binding agents to inhibit the activity of DNA helicases is not without precedence. Similar effective inhibition of the unwinding of DNA by the BLM and Werner\'s DNA helicases by the minor groove binder distamycin A has been observed. Further, and similar to RecBCD, interc
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DGK is not the only DGK isoform that
2020-11-02

DGKε is not the only DGK isoform that has been associated with p53. It has been shown that DGKζ binds to p53 and modulates its activity in both the cytoplasm and the nucleus [39]. In the cytosol DGKζ promotes the degradation of p53 through the ubiquitin-proteosome system [39], also a likely mechanis
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br Cysteine proteases as molecular targets for trypanosomati
2020-11-02

Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these st
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Testosterone is inactivated through hydroxylation and conjug
2020-11-02

Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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br Results br Discussion br Experimental
2020-11-02

Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p
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br Nuclear export and the
2020-11-02

Nuclear export and the functions of CRM1 The nuclear envelope provides a compartmentalized intracellular environment for DNA replication, the synthesis of RNA, and production of ribosomes, and, as such, it can regulate cellular biological processes including apoptosis and proliferation. Nucleocyt
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The objective of the present
2020-11-02

The objective of the present study was to investigate the role of the CRF system in the neuroadaptations associated with nicotine dependence. To this aim, the regulation of the gene expression of CRF and its receptors was assessed in agomelatine synthesis regions belonging to the reward pathway usin
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br Theory br Method To test our hypotheses as
2020-11-02

Theory Method To test our hypotheses as shown in Fig. 1, we conducted a survey at an international media company (hereafter referred to as ‘MediaCo’) headquartered in the UK. Its 5500 employees are dispersed throughout the world, partly due to massive acquisitions within the past decade. In ex
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br The modulation of ER from SERMs to
2020-11-02

The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective AT13148 receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despite
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br The ubiquitin proteasome system The
2020-10-31

The ubiquitin proteasome system The ubiquitin proteasome system (UPS) plays a significant role in the regulation of cell growth and survival, in addition to maintaining cellular homeostasis. By means of the UPS, n-acetyl-l-cysteine can precisely and temporally degrade approximately 80% of the en
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