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Among the Ub interactions observed
2019-10-11
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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In general cellular senescence is considered a programmed re
2019-10-11
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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fusidic acid mass During the past three decades platinum bas
2019-10-11
During the past three decades, platinum-based DNA-alkylating agents have been employed in the treatment of various cancers [14]. Oxaliplatin is currently used as a first-line treatment for colorectal cancer (CRC) [15]. Unfortunately, a large portion of CRC patients receiving oxaliplatin-based chemot
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DL-α-Hydroxyglutaric acid disodium salt br Biological roles
2019-10-11
Biological roles of DGKϵ Summary and future perspectives The most DL-α-Hydroxyglutaric acid disodium salt segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheless, the se
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We also discovered important clues to domain binding
2019-10-11
We also discovered important clues to domain MJ33 lithium salt of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region
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We have reported previously that aminoacrylate derivatives
2019-10-11
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHODH).
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In this study using REMD with the
2019-10-11
In this study, using REMD with the crystal environment, we investigate the effect of cryo-cooling on the crystal structure of Escherichia coli DHFR. DHFR is an important model enzyme (for review, see, e.g., (30)), and has been studied for decades (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43).
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In mouse lung arsenite enhances the
2019-10-11
In mouse lung, arsenite enhances the formation of cigarette smoke-induced 8-oxodeoxyguanine (Hays et al., 2006) and BaP-induced DNA adducts (Evans et al., 2004). Moreover, arsenite inhibits the repair of BaP-induced DNA adducts in human lung carcinoma A549 EPZ004777 (Schwerdtle et al., 2003), indic
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We found that the postnatal
2019-10-10
We found that the postnatal absence of norepinephrine yields differing effects depending on noradrenergic receptor type and Tazobactam sodium salt region. The density of α1-AR, indicated by [3H]prazosin binding was similar between Dbh+/− and Dbh−/− mice except for a significant increase in hippocam
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Conoidin A and br Materials and methods br Results br Discus
2019-10-10
Materials and methods Results Discussion Conflict of interest Introduction Dopamine-β-hydroxylase (DβH) deficiency is a rare autosomal recessive disorder characterized by the congenital absence of DβH, the enzyme converting dopamine to noradrenaline in sympathetic nerve terminals and
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These reactions are used to account for
2019-10-10
These reactions are used to account for variations in protein solubility or vesicle recovery. For example, with DGKθ we have found it necessary to maintain the purified enzyme in a solution of 0.01% DDM (DGK-D dilution buffer) in the control reaction to prevent enzyme loss due to aggregation or adhe
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Preparation of the regioisomeric pyridooxazepinones and was
2019-10-10
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and Cyclophosphamide chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1
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Recent pharmaceutical research in the field of respiratory
2019-10-10
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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In conclusion our work provides the preclinical evidence
2019-10-10
In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer Ketorolac pathway and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for t
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Compounds were synthesized as illustrated in tetrazole yl be
2019-10-10
Compounds – were synthesized as illustrated in , , , , . 3-(1-tetrazole-5-yl)benzaldehyde was obtained in 95% yield via [2+3] cycloaddition of sodium azide to commercially available 3-cyanobenzaldehyde in presence of triethylamine as reported in the literature. Nitration of 3-hydroxyacetophenone wi
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