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The photocleaving properties of were studied
2021-06-28
The photocleaving properties of 1 were studied by performing ΦX174 photocleavage assays. Light irradiation of the mixtures of increasing amounts of 1 with supercoiled DNA caused>90% supercoiled form relaxation and approximately 5% of linearization for the higher concentrations of 1 (1:10bp and 1:2bp
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Indeed the alkyl group is not
2021-06-28
Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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Our finding that activating DDR variants are a cause of
2021-06-28
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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The transcriptome analysis of barley seeds in two tissue fra
2021-06-28
The transcriptome analysis of barley seeds in two tissue fractions: starchy endosperm/aleurone and embryo/scutellum, during maturation, desiccation and germination, revealed the large group of GA-responsive genes (Sreenivasulu et al., 2008). These transcripts have been divided into two groups. Nearl
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By live imaging of GUL GFP
2021-06-28
By live imaging of GUL-1-GFP, we observed the kinetics of aggregate movement within the cell. One of the marked characteristics of GUL-1-GFP cytosolic (but not nuclear-associated) aggregate motion was a “comet-like” movement that was found to be dependent on the presence of properly polymerized micr
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In recent years there has been
2021-06-25
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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Fusion genes are formed as the result
2021-06-25
Fusion genes are formed as the result of either structural chromosomal rearrangement including, primarily, translocation, inversion, amplification and deletion, or non-structural aberrations caused by cis- and trans-splicing or transcriptional read-through. Such events are known to play important ro
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br Methods br Results and discussion br Conclusions br
2021-06-25
Methods Results and discussion Conclusions Conflict of interest Acknowledgment The research is supported by the National Natural Science Foundation of China (Grant No. U1603285). Overview of the MAPK pathway The mitogen-activated protein kinases (MAPK) pathway, often known as a ca
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Among RAS mutant tumors analyzed
2021-06-25
Among RAS mutant tumors analyzed, we found that the efficacy of either the SHP2 inhibitor SHP099, or combined MEK and SHP2 inhibition was best in those expressing RAS mutations at G12 (Figure 7B). Recent studies revealed that cellular RAS(G12C) activity depends on RTK-mediated nucleotide exchange, a
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Prostaglandin E PGE is involved in several biological proces
2021-06-25
Prostaglandin E2 (PGE2) is involved in several biological processes such as renal function, inflammation, angiogenesis, and tumor growth. The various biological effects of PGE2 are mediated by the so-called E-type prostanoid receptors (EP1 to EP4). Among these, the EP4 receptor has been well studied
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The synthetic routes to the substrates based
2021-06-25
The synthetic routes to the substrates based on the 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene cores are depicted in Scheme 3. A Michael-type glycosylation of 2,3-dihydroxynaphthalene 16a gave the acetylated sugar 17a which was deprotected giving the required β-glucosidase sub
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Among the Ub interactions observed in the HOIP structure is
2021-06-25
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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br Ubiquitin Capture by the Mobile APC
2021-06-25
Ubiquitin Capture by the Mobile APC11 RING Domain Contributes to Processive Substrate Ubiquitylation Although the rules of Ub-mediated proteolysis are only beginning to emerge, the rate and order in which different APC/C substrates are degraded during the alcohol dehydrogenase inhibitor correlat
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A key inciting event in atherosclerosis is the deposition of
2021-06-25
A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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Currently much effort has been made to design and synthesize
2021-06-25
Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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