1,724,367 research outputs found
A Concise Route to MK-4482 (EIDD-2801) from Cytidine: Part 2
No full textA new route to MK-4482 (1) was developed. The route
replaces uridine with the more available and less expensive cytidine. Low cost, simple reagents are used for the
chemical transformations and the yield is improved from 17% to 44%. A step is removed from the longest linear
sequence, and these advancements are expected to expand access to MK-4482
should it become a viable drug substance
A Concise Route to MK-4482 (EIDD-2801)
No full textA two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an
esterification and hydroxamination of cytidine.
The reactions can be conducted in either order with overall yields of
67% (first step—esterification) and 37% (first step—hydroxamination). Selective
esterification of the nucleoside’s primary alcohol by enzymatic means
eliminated the need for diol protection/deprotection, and direct transamination
with hydroxylamine precluded the necessity of activating the nucleobase for
amine coupling. This results in a significant
advancement over the reported synthesis which is formed in at best 17%
yield. The step count is reduced from
five transformation to two, and the more expensive uridine is replaced with the
more available cytidine
4482. Procédure de canonisation de Jeanne d'Arc
No full text4482. Procédure de canonisation de Jeanne d'Arc. In: Molinier Auguste. Les Sources de l'histoire de France - Des origines aux guerres d'Italie (1494). IV. Les Valois, 1328-1461. Paris : A. Picard et fils, 1904. p. 318
Linked collectors and determiners for: Taxonomic and morphological studies on the Lygephila dorsigera (Walker, 1865) species-group, with description of a new species (Lepidoptera, Erebidae, Toxocampinae).
No full textNatural history specimen data linked to collectors and determiners held within, "Taxonomic and morphological studies on the Lygephila dorsigera (Walker, 1865) species-group, with description of a new species (Lepidoptera, Erebidae, Toxocampinae)". Claims or attributions were made on Bionomia by volunteer Scribes, <a href="http://bionomia.net/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92">https://bionomia.net/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92</a> using specimen data from the dataset aggregated by the Global Biodiversity Information Facility, <a href="https://gbif.org/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92">https://gbif.org/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92</a>. Formatted as a Frictionless Data package
Linked collectors and determiners for: Taxonomic and morphological studies on the Lygephila dorsigera (Walker, 1865) species-group, with description of a new species (Lepidoptera, Erebidae, Toxocampinae).
No full textNatural history specimen data linked to collectors and determiners held within, "Taxonomic and morphological studies on the Lygephila dorsigera (Walker, 1865) species-group, with description of a new species (Lepidoptera, Erebidae, Toxocampinae)". Claims or attributions were made on Bionomia by volunteer Scribes, <a href="http://bionomia.net/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92">https://bionomia.net/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92</a> using specimen data from the dataset aggregated by the Global Biodiversity Information Facility, <a href="https://gbif.org/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92">https://gbif.org/dataset/89078bb1-2ca1-4482-bdc1-7bf883609e92</a>. Formatted as a Frictionless Data package
A Concise Route to MK-4482 (EIDD-2801) from Cytidine: Part 2
No full text© 2021 Georg Thieme Verlag. All rights reserved. A new route to MK-4482 was developed. The route replaces uridine with the more available and less expensive cytidine. Low-cost, simple reagents are used for the chemical transformations, and the yield is improved from 17% to 44%. A step is removed from the longest linear sequence, and these advancements are expected to expand access to MK-4482 should it become a viable drug substance
miR-4482 and miR-3912 aim for 3'UTR of ERG mRNA in prostate cancer.
No full textEts-related gene (ERG) is overexpressed as a fusion protein in prostate cancer. During metastasis, the pathological role of ERG is associated with cell proliferation, invasion, and angiogenesis. Here, we hypothesized that miRNAs regulate ERG expression through its 3'UTR. Several bioinformatics tools were used to identify miRNAs and their binding sites on 3'UTR of ERG. The selected miRNAs expression was analyzed in prostate cancer samples by qPCR. The miRNAs overexpression was induced in prostate cancer cells (VCaP) to analyze ERG expression. Reporter gene assay was performed to evaluate the ERG activity in response to selected miRNAs. The expression of ERG downstream target genes was also investigated through qPCR after miRNAs overexpression. To observe the effects of selected miRNAs on cell proliferation and migration, scratch assay was performed to calculate the cell migration rate. miR-4482 and miR-3912 were selected from bioinformatics databases. miR-4482 and -3912 expression were decreased in prostate cancer samples, as compared to controls (p<0.05 and p<0.001), respectively. Overexpression of miR-4482 and miR-3912 significantly reduced ERG mRNA (p<0.001 and p<0.01), respectively) and protein (p<0.01) in prostate cancer cells. The transcriptional activity of ERG was significantly reduced (p<0.01) in response to miR-4482 and-3912. ERG angiogenic targets and cell migration rate was also reduced significantly (p<0.001) after miR-4482 and -3912 over-expression. This study indicates that miR-4482 and -3912 can suppress the ERG expression and its target genes, thereby, halt prostate cancer progression. These miRNAs may be employed as a potential therapeutic target for the miRNA-based therapy against prostate cancer
mRNA expression of ERG targets genes altered in miR-4482 and miR-3912 transfected HUVEC.
No full textmRNA expression of ERG targets genes altered in miR-4482 and miR-3912 transfected HUVEC.</p
- …
