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The compounds were ranked based on
2020-02-22
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR a
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br Introduction Noncanonical nucleoside triphosphates
2020-02-22
Introduction Noncanonical nucleoside triphosphates (NTPs; such as deoxyinosine triphosphate (dITP), deoxyxanthosine triphosphate (dXTP), 8-oxo-deoxyguanosine triphosphate, and 2-oxo-deoxyadenosine triphosphate are produced from oxidation, deamination, or other modifications of canonical nucleotid
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After crown formation root development
2020-02-21
After crown formation, root development begins via the interaction between the Hertwig root sheath (HERS) and the dental papilla, which differentiates into odontoblasts and forms dentin and pulp. HERS is associated with the number of roots and their morphology . The stem cells from the apical papill
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In this contribution herein we report our newly devised
2020-02-21
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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The folate pathway plays an essential role in
2020-02-21
The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec
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The inhibition of FAS by C
2020-02-21
The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi
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Cot MAP K is the sole MAP
2020-02-21
Cot (MAP3K8) is the sole MAP3K that activates the MEK1/2-Erk1/2 following the activation of the TLR/IL-1 receptor superfamily as well as some receptors of the TNF receptor family [8], [9], [10] and mediates the production of chemokines and cytokines in different cell systems [reviewed in [11]]. Thus
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br Atypical collagen glycosylation The
2020-02-21
Atypical collagen glycosylation The disaccharide Glc(α1-2)Gal(β1-O) decorating collagens is strongly conserved across the animal kingdom, yet for every rule, nature provides exceptions. The deep-sea worm Riftia pachyptila of the phylum Annelida represents an intriguing exception. R. pachyptila is
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Hinokitiol has versatile abilities as anticancer antimicrobi
2020-02-21
Hinokitiol has versatile abilities as anticancer, antimicrobial and molecule transport agents and appears to have no developmental toxicity or carcinogenic effects (Imai et al., 2006b). For anticancer activities, it causes apoptosis and transferases arrest in many different types of cancers, such as
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br Conflict of interest br Supplementary
2020-02-21
Conflict of interest Supplementary methods and materials Acknowledgments This work was supported by an Early Career Researcher grant awarded by the Institute of Health and Biomedical Innovation to IMW and Queensland University of Technology, and grants awarded to SS by the Prostate Cancer F
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ER redox imbalance leads to the accumulation of misfolded pr
2020-02-21
ER redox imbalance leads to the accumulation of misfolded proteins, which might trigger the unfolded protein response (UPR) [17]. In the initiation of UPR, GRP78 preferentially binds to unfolded proteins, shifting the binding equilibrium away from IRE-1, PERK, and ATF-6, the initiators of UPR [18].
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br Multi subunit RINGs There are RING type E s
2020-02-21
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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br Results and discussion br Conclusion In the current study
2020-02-21
Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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The occurrence of three Ag NORs per metaphase
2020-02-21
The occurrence of three Ag-NORs per metaphase and/or a maximum of three nucleoli per nucleus in most of the varieties may be explained by chromosomal rearrangements or unequal crossing-over events that induce the deletion of the fourth active rDNA loci. Also, the chromosome pair that showed less int
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DNA damage represents a persistent threat to genomic stabili
2020-02-21
DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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