4869-46-9Relevant articles and documents
Enantioselective Synthesis of D -α-(Uracil-5-yl)glycine Derivatives and Their Racemization-Free Incorporation into a Model Peptide
Weckenmann, Nicole M.,Nachtsheim, Boris J.
, p. 6624 - 6630 (2015)
An efficient asymmetric synthesis of D-α-(uracil-5-yl)glycine derivatives using an enzymatic dynamic kinetic resolution of D,L-hydantoin intermediates with an immobilized D-hydantoinase (D-Hyd-1) is described. In addition, mild conditions for a racemization-free solid-phase peptide synthesis (SPPS) using the Fmoc strategy have been found.
A structure-specific small molecule inhibits a miRNA-200 family member precursor and reverses a type 2 diabetes phenotype
Abegg, Daniel,Adibekian, Alexander,Aikawa, Haruo,Disney, Matthew D.,Haniff, Hafeez S.,Knerr, Laurent,Lemurell, Malin,Liu, Xiaohui,Meyer, Samantha M.,Tong, Yuquan
, p. 300 - 10,311 (2022/02/17)
MicroRNA families are ubiquitous in the human transcriptome, yet targeting of individual members is challenging because of sequence homology. Many secondary structures of the precursors to these miRNAs (pri- and pre-miRNAs), however, are quite different. Here, we demonstrate both in vitro and in cellulis that design of structure-specific small molecules can inhibit a particular miRNA family member to modulate a disease pathway. The miR-200 family consists of five miRNAs, miR-200a, -200b, -200c, -141, and -429, and is associated with type 2 diabetes (T2D). We designed a small molecule that potently and selectively targets pre-miR-200c's structure and reverses a pro-apoptotic effect in a pancreatic β cell model. In contrast, an oligonucleotide targeting the RNA's sequence inhibited all family members. Global proteomics and RNA sequencing analyses further demonstrate selectivity for miR-200c. Collectively, these studies establish that miR-200c plays an important role in T2D, and small molecules targeting RNA structure can be an important complement to oligonucleotides.
The arylimines of 2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbaldehyde: Synthesis and their application in 1,3-dipolar cycloaddition reaction
Osyda, Dominika,Motyka, Radoslaw,Walczak, Krzysztof Z.
body text, p. 1280 - 1284 (2010/03/23)
(Chemical Equation Presented) A number of aldimines have been obtained in very good yield in reaction of 5-formyl-1,3-dimethyluracil with various substituted anilines in boiling methanol. Selected aldimines were treated with nitrile oxides generated from 4-chlorobenzaldoxime or 4-methylbenzaldoxime forming the appropriate 1,3-cycloadducts in moderate yields.
