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br Results br Discussion Adaptive drug resistance is
2020-10-21
Results Discussion Adaptive drug resistance is a major challenge to the clinical success of cancer therapies. Incomplete inhibition of oncogenic signaling allows survival of “drug-tolerant” tumor cells, which persist in that state for variable periods before acquiring additional genetic mutati
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br Conclusion The past few years have
2020-10-21
Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte
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CAA is a carcinogenic metabolite of vinyl chloride
2020-10-21
CAA is a carcinogenic metabolite of vinyl chloride, forming several different DNA adducts including the cyclic sirtuin adducts 3,N4-ethenocytosine (εC), 1,N6-ethenoadenine (εA), N2,3-ethenoguanine (εG), and 1,N2-ethenoguanine (1,N2-εG), with the A and C cyclic adducts the most predominant, and all
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We recently reported that the
2020-10-21
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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As a functional ETC is required for DHODH catalysis Loffler
2020-10-21
As a functional ETC is required for DHODH catalysis (Loffler, Jockel, Schuster, & Becker, 1997; Rawls, Knecht, Diekert, Lill, & Loffler, 2000; Zameitat, Freymark, Dietz, Loffler, & Bolker, 2007), DHODH depends on the mitochondrial ETC to generate adequate concentrations of ubiquinone (Fig. 2). Cells
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Reports on the participation of NDH along
2020-10-21
Reports on the participation of NDH2 along with other respiratory complexes in the formation of a large supercomplex (Grandier-Vazeille et al. 2001) or even a respirosome-like structure in S. cerevisiae mitochondria (Matus-Ortega et al. 2015) are very intriguing. Similarly, in Y. lypolytica mitochon
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The phenolic hydroxyl group of ezetimibe tolerated various s
2020-10-21
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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Atglistatin At first cartilage damage in osteoarthritis refl
2020-10-20
At first, cartilage damage in osteoarthritis reflects the loss of proteoglycan and collagen network that increases the swelling of tissues. The incremented expression of DDR2 receptor has also co-related with the depletion of cartilage in surgically induced OA model [8]. Osteoarthritis, a degenerati
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br A brief introduction to DUBs
2020-10-20
A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating Dihydroeponemycin (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be classif
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Common enzyme quantitative methods include enzyme
2020-10-20
Common enzyme quantitative methods include enzyme-linked immunosorbent assay [,] (ELISA), chemiluminescence (CLIA) [, , ] and immunochromatography []. The advantages of ELISA are cost reduction and automation, but non-specific reaction caused by HOOK effect, false positive caused by cross-contaminat
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One of the most frequent gene alterations in
2020-10-20
One of the most frequent gene alterations in MM is methylation of the p15 and p16 genes in the 5′ upstream region. P15 and p16 proteins are Trimidox regulators involved in the inhibition of transition from G1 to S phase. Frequencies of p15 or p16 gene methylation up to 32% and 53%, respectively, ha
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The androgen receptor AR is a steroid hormone
2020-10-20
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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Materials and methods br Results br
2020-10-20
Materials and methods Results Discussion Microbial production of trans-4Hyp, an added-value amino nmda receptor antagonist for pharmaceuticals, offers significant advantages over conventional chemical extraction in economic and environmental aspects. However the low titer and productivity wi
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It has been shown that CK
2020-10-20
It has been shown that CK1δ phosphorylates α-, β- and γ-tubulin in vitro and that CK1δ specifically interacts with the trans Golgi network, COPI positive vesicles, and centrosomes in interphase cells [11], [12], [13], [14]. Moreover CK1δ is also associated with granular particles that are associated
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Since the aggregation of neurotoxic forms
2020-10-20
Since the aggregation of neurotoxic forms of Aβ plays a pivotal role in AD pathogenesis, an approach that using small molecules to bind Aβ monomers and prevent their assembly into cytotoxic oligomers attracts great interest for the development of AD drugs. Therefore, the potential inhibitory activit
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