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This study demonstrates that GUL affects multiple pathways
2021-04-29

This study demonstrates that GUL-1 affects multiple pathways/processes. As GUL-1 is likely to function as an RNA-binding protein, it is conceivable that the mRNAs involved are bound to GUL-1 as part of the regulatory function of the protein. In fact, in S. cerevisiae Ssd1 was shown to bind multiple
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Not all of the biological activities exhibited
2021-04-28

Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the Dynorphin (2-17), amide, porcine is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability o
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2hcl br Allosteric inhibitors In general
2021-04-28

Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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br Disclosure statement br Acknowledgment This work
2021-04-28

Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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br Cytochrome P monooxygenases Cytochrome P monooxygenases P
2021-04-28

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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Swainsonine br Results br Discussion In
2021-04-28

Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Swainsonine via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inh
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Although the reasons why viral
2021-04-28

Although the reasons why viral RNA does not bind to and activate PKR in WNV-infected cells are not known, some of the known characteristics of flavivirus infections provide possible clues. The viral hiv protease inhibitors protein forms dimers that associate with ER membranes and viral RNA (Lindenba
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A second advance came with the discovery
2021-04-28

A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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br DNA end processing enzymes
2021-04-28

DNA end processing enzymes The simplest DSB is one that consists of two blunt DNA ends as these termini can be re-joined without processing. However, DSBs induced by ionizing radiation and reactive oxygen species are notorious for producing DNA ends which are non-ligatable (“dirty ends”) and thus
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Sequence alignment of cfALDH with the human ALDH indicates t
2021-04-28

Sequence alignment of cfALDH with the human ALDH1 indicates that the cyanobacterial protein contains the same GQCC motif as the human ALDH1 and ALDH2 proteins [24] (Fig. 1d, highlighted in red, and Supplementary Fig. 2). This motif is present in ALDH1/2 orthologues and these residues reside at the b
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br Materials and methods br Results The frequency of hyperme
2021-04-27

Materials and methods Results The frequency of hypermethylation of RARbeta, RASSF1A, FHIT, GSTP1, MGMT, VHL and DAPK in patients with primary LSCC was assessed in both the tumor tissue samples and macroscopically and histologically normal mucosa from distant sites of the surgical specimen, ubi
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1 78 As previously reported azole class
2021-04-27

As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Given a disruption of membrane internalization and an increa
2021-04-27

Given a disruption of membrane internalization and an increase in synaptic glutamate receptors in CPG2 knockdown neurons, one might expect an increase in dendritic spine size as membrane continues to be inserted into the spines during receptor exocytosis. However, we observed the opposite phenotype,
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Udenafil also has shown the ability to significantly
2021-04-27

Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models when
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Together the data suggests that more work
2021-04-27

Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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