Role of JMJD3 Demethylase and Its Inhibitor GSK-J4 in Regulation of MGMT, TRA2A, RPS6KA2, and U2AF1 Genes in Prostate Cancer Cell Lines was written by Sanchez, Anna;El Ouardi, Driss;Houfaf Khoufaf, Fatma Zohra;Idrissou, Mouhamed;Boisnier, Tiphanie;Penault-Llorca, Frederique;Bignon, Yves-Jean;Guy, Laurent;Bernard-Gallon, Dominique. And the article was included in OMICS in 2020.Application In Synthesis of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate The following contents are mentioned in the article:
To provide evidence on involvement of JMJD3 demethylase in prostate tumor progression, & particularly on MGMT, TRA2A, RPS6KA2, & U2AF1 candidate gene expressions, anal. of H3K27me3 enrichment was performed by chromatin immunoprecipitation (ChIP)quant. polymerase chain reaction (qPCR) after inhibition of JMJD3 by GSK-J4 in prostate cancer cell lines. Subsequently, reverse transcription (RT)-qPCR conducted after inhibition of JMJD3 by siRNA/GSK-J4 inhibitor demonstrating its demethylase activity on expression of studied genes. In addn, inhibition of JMJD3 by siRNA was validated by Western blotting. Results: gene expression by RTqPCR anal. after inhibition of JMJD3 by siRNA & chem. inhibition by GSK-J4. JMJD3 inhibition by GSK-J4 exhibited non-vital decrease in JMJD3 expression in the 3 cell lines LNCaP, DU-145 & PC-3. The mRNA anal. confirmed that enrichment in H3K27me3 on target genes, led to an inhibition of MGMT, TRA2A, RPS6KA2, & U2AF1 exprsn, affirming H3K27me3 as a repressive epigenetic marker. Conclusion: The data anal. emphasized the link between JMJD3 and regulation of these genes in prostate cancer cell lines. JMJD3, regulated in vitro by siRNA/GSK-J4, making JMJD3 a potential therapeutic target. In future, it would be interesting to see effect of JMJD3 inhibition on those genes in vivo. This study involved multiple reactions and reactants, such as Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0Application In Synthesis of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate).
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate (cas: 1373423-53-0) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application In Synthesis of Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia