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A novel series of DHODH inhibitors
2020-12-30

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Quinacrine hydrochloride hydrate receptor The present study
2020-12-30

The present study provides the first evidence that the human uroepithelial Quinacrine hydrochloride hydrate receptor in vitro respond directly, within 48h, to this carcinogen by promoting extensive vacuolation and DAPK expression. By using the TEM, ICC and Western blotting, we found that the arseni
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Atg cleaves Atg at the peptide
2020-12-30

Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated At
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In this review we first introduce the in
2020-12-30

In this review, we first introduce the in vivo metabolism profile of VD3, and the mediation of Cyp3a gene transcription by PXR and CAR in humans, mice and rats. We then focus on the species-specific VDR-dependent regulation of human (CYP3A4, CYP3A5 and CYP3A7), mouse (mainly CYP3A11 and CYP3A13), an
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On the basis of the findings described above a
2020-12-30

On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed
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By using the C elegans Matrisome Annotator tool
2020-12-30

By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome caffeic acid in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome for v
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br Clinical studies br Practical implications for young
2020-12-30

Clinical studies Practical implications for young women Conclusion Research on the oncogenic mechanism of hormones has advanced dramatically in the latter years. The finding that progestogens are more powerful determinants of risk than estrogens in breast cancer has been added to advances
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The expression profiles of NCK and ABI genes after ESC
2020-12-30

The expression profiles of NCK and ABI genes after ESC bacterial infection were determined. As shown in Fig. 1a, NCK1, ABI2a and ABI2b were significantly induced after ESC infection. While, ABI3a was significantly downregulated. Intestine was confirmed as a site of E. ictaluri entry by bacteriologic
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Current therapeutic protocols in OS
2020-12-30

Current therapeutic protocols in OS and ES consist of neoadjuvant chemotherapy and local surgical resection, followed by adjuvant chemotherapy. These treatments lead to a 70% overall survival for localized disease but can decrease to 15% in case of metastasis. With CS being resistant to conventional
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The applications of fungal enzymes in paper industry involve
2020-12-30

The applications of fungal enzymes in paper industry involve biobleaching of pulp, pulp de-inking, degradation of dissolved and suspended organic compounds in concentrated effluents of mills and enhanced fibrillation. Enzymes usage is encouraged in paper industry in order to reduce the use of chemic
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The potential impact of multiple washings
2020-12-30

The potential impact of multiple washings on DNA retention in semen stains had not previously been addressed. In the present study, multiple washes of semen-stained cotton cloth produced only a minimal loss of recovered DNA suggesting that multiple washes may not materially affect DNA recovery (Fig.
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br Materials and methods Male Hartley guinea pigs g
2020-12-29

Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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br Clinical trials of CRM inhibitors KPT clinical trials
2020-12-29

Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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soluble guanylate cyclase Ethyl naphthoates a h were success
2020-12-29

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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In vitro studies suggest that cPLA
2020-12-29

In vitro studies suggest that cPLA2α does not show clear preference for the headgroup present at the sn-3 position, although a slight preference for zwitterionic phospholipids such as PC and PE has recently been pointed out [24]. In this regard, mass spectrometry analyses of glycerophospholipid hydr
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