Design, synthesis, anticancer evaluation, molecular docking and cell cycle analysis of 3-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine derivatives as potent histone lysine demethylases (KDM) inhibitors and apoptosis inducers.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.102929
Abstract: A novel series of pyrazolo[1,5-a]pyrimidines were synthesized and proved by their spectral and elemental analysis, some elected of the newly synthesized compounds were examined for their cytotoxic activity employing MTT assay on two cancer cell… read more here.
Keywords: histone lysine; analysis; lysine demethylases; cell cycle ... See more keywords
Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114143
Abstract: Post-translational modifications (PTMs) of histone by histone demethylases (KDMs) play an important role in the regulation of gene expression, which implicates the development of various human cancers and other diseases. Discovering and developing inhibitors targeting… read more here.
Keywords: histone; lysine demethylases; lysine; drug discovery ... See more keywords
Cancer-associated 2-oxoglutarate analogues modify histone methylation by inhibiting histone lysine demethylases.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2018.06.048
Abstract: Histone lysine demethylases (KDMs) are 2-oxoglutarate-dependent dioxygenases (2-OGDDs) that regulate gene expression by altering chromatin structure. Their dysregulation has been associated with many cancers. We set out to study the catalytic and inhibitory properties of… read more here.
Keywords: associated oxoglutarate; histone lysine; lysine demethylases; cancer ... See more keywords
Lysine Demethylases: Promising Drug Targets in Melanoma and Other Cancers
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Genetics"
DOI: 10.3389/fgene.2021.680633
Abstract: Epigenetic dysregulation has been implicated in a variety of pathological processes including carcinogenesis. A major group of enzymes that influence epigenetic modifications are lysine demethylases (KDMs) also known as “erasers” which remove methyl groups on… read more here.
Keywords: drug targets; melanoma cancers; demethylases promising; lysine demethylases ... See more keywords