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Our observation that nuclear but not cytoplasmic EP expressi
2021-01-08

Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant Parecoxib Sodium whereas cytoplasmic EP4 was commonly observed [13]. While G protein-cou
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br Materials and methods br Results br Discussion Ubiquitina
2021-01-08

Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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br Conclusions The PQQ dependent CcPDH is the first PQQ
2021-01-08

Conclusions The PQQ-dependent CcPDH is the first PQQ-dependent enzyme identified in eukaryotes. The PQQ cofactor binds the enzyme with high affinity, reflected in a Kd of 1.1 nM, and the enzyme oxidizes 2KG, l-fucose, and rare sugars such as d-arabinose and l-galactose. The AA8 cytochrome b domai
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Besides degrading cholesterol the cholesterol degradation pa
2021-01-08

Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market
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A number of immune relevant
2021-01-08

A number of immune-relevant genes have been studied to explore the immunologic mechanisms in large yellow croakers; however, the chemokine receptor CXCR family has never been studied in this organism. Chemokines are a large superfamily of chemotactic cytokines that are utilized to direct the traffic
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br Materials and methods br Results and discussion In
2021-01-08

Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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br Experimental br Declaration of interest
2021-01-07

Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR AVL-292 library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was modified and
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CSN was initially identified based on the constitutitvely ph
2021-01-07

CSN was initially identified based on the constitutitvely photormophogenic (cop) mutants from Arabidopsis thaliana [48]. csn mutants are Cullin deneddylation-deficient, consequently accumulate neddylated Cullins, and arrest growth shortly after germination [49, 50, 51]. Weak csn mutants have defects
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br The central role of
2021-01-07

The central role of DNA-PK in the NHEJ NHEJ can be divided in several steps (Fig. 1A): 1) recognition and binding of Ku at each ends of the DSB following by the assembly of the DNA-PK at the break points and bridging; 2) phosphorylation of the DNA ends by DNA-PKcs; 3) ligation of the ends by DNA
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R 568 hydrochloride A set of small molecule LigI inhibitors
2021-01-07

A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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There exists a glucose residue in the structure of Acid
2021-01-07

There exists a glucose residue in the structure of 5. Acid hydrolysis (Supplementary data) followed by TLC comparison with the reference compound as well as GC–MS analysis (l-cysteine methyl ester hydrochloride derivative: tR=22.22min for glucose residue of 5 and 22.46min for the reference compound)
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Uracil residues incorporated into DNA exist transiently sinc
2021-01-07

Uracil residues incorporated into DNA exist transiently since they are subject to removal by the multi-step uracil-initiated DNA SCR7 excision repair (BER) process [2], [14]. In E. coli, uracil-DNA BER is initiated by uracil-DNA glycosylase (Ung), which catalyzes the hydrolytic cleavage of the N-gl
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During DNA replication p protein binds PCNA in its role
2021-01-07

During DNA replication p21 protein binds PCNA, in its role as processivity factor, to stop replication when there is DNA damage, and apparently p21 also binds PCNA when this is in complex with Cyc/CDKs [11]. In plants, KRPs (functional analogs of p21), inhibit kinase activity in CycD/CDKs complexes
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From the general synthetic route we first
2021-01-07

From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Chemistry Scheme shows the synthesis
2021-01-07

Chemistry Scheme 1 shows the synthesis of compounds 15-1–15-33 from commercially available 2-(4-aminophenyl)acetonitrile (8a). Protection of the starting material 8a with di-t-butyl dicarbonate afforded 9. The reaction of 9 with methyl 1-chloroisoquinoline-4-carboxylate in the presence of sodium
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