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In this contribution herein we
2021-06-18

In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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br Conclusions This report describes the discovery
2021-06-17

Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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An even more striking difference is observed when comparing
2021-06-17

An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97
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To date methods for the simultaneous analysis
2021-06-17

To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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Six substrate recognition sites SRS SRS
2021-06-17

Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh's proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two addi
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The X ray crystal structure of palbociclib bound to CDK
2021-06-17

The X-ray crystal structure of palbociclib bound to CDK6 without a azacytidine (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V complex. I
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To estimate the nonparametric regression
2021-06-17

To estimate the nonparametric regression, we use a B-spline basis. Let be the space of polynomial splines of degree and denote a normalized B-spline basis with and , where is the supremum norm. For any and , we have for some coefficients . Here we allow to increase with and differ for differ
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Within the cluster of North African populations the Sousse p
2021-06-17

Within the cluster of North African populations the Sousse population sample is somewhat different from the other six populations. One has to analyze more in depth the reasons of this isolation that has been shown by other genetic studies (Fadhlaoui-Zid et al., 2015). It seems that the particular ge
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Some limitations of this study
2021-06-17

Some limitations of this study must be noted. First, since the pretransplant evaluation of the T-cell immune response was performed just before transplantation, we cannot establish whether samples obtained at different times before the transplant would offer similar results, since end terminal disea
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Recent studies showed that the activity of CK was
2021-06-17

Recent studies showed that the activity of CK2 was significantly reduced in ischemic stroke model rats, and cerebral I/R injury significantly decreased the expression of CK2α (Lee et al., 2004; Kim et al., 2012; Zhou et al., 2016). In addition, the dysregulation of CK2 is involved in ERS/UPR in non-
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Based on the above we hypothesized that a
2021-06-17

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Interestingly increased level of both circulating ET and
2021-06-17

Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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Taking all the data together we
2021-06-17

Taking all the data together, we propose the possible mechanism of glyphosate-induce cell proliferation via estrogen receptor signaling (Fig. 10). Glyphosate may bind to ERα followed by an activation step that starts with the phosphorylation of ERα and activation of other signaling proteins by phosp
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Studies of nuclear transplantation of diploid
2021-06-17

Studies of nuclear transplantation of diploid imprint-free PGCs have shown that the reconstituted oocytes developed to day 9.5 of gestation, with severely retarded embryos and abnormal placentae (Kato et al., 1999). We also reported that MII oocyte injection of imprint-free phESCs without imprinted
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br Conflict of interest br Acknowledgments This work was
2021-06-17

Conflict of interest Acknowledgments This work was supported in part by grants from the , Spain (INCITE08PXIB203092PR). VGM was supported by a FPU pre-doctoral scholarship from the , Spain. MLR was supported in part by a crowdfunding campaign (PRECIPITA), coordinated by the Spanish Foundation
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