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The α-ketoglutarate-dependent (AlkB) superfamily of FeII/2-oxoglutarate (2-OG) -dependent dioxygenases consists of a unique class of nucleic acid repair enzymes which reversibly remove alkyl substituents from nucleobases through oxidative dealkylation. Recent studies have verified the involvement of AlkB dioxygenases in a variety of human diseases. However, the development of small organic molecules that can function as enzyme inhibitors to block the action of oxidative dealkylation is still in its infancy. These purposeful chemical motifs, if capable of influencing the dealkylation activity, would have a potential clinical value by controlling genetic information expression. In this Perspective, we will summarize some of the most updated inhibitors of AlkB family demethylases, and hope to provide a thought for the follow-up screening optimization.
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A family of alpha- KETOGLUTARIC ACID and Fe(II)-dependent dioxygenases that are homologous to AlkB, an enzyme that repairs alkylated nucleic acids in E. coli. The mammalian homologs have diverse substrate specificities and functions that include DNA REPAIR, generating unique wobble modifications in URIDINE tRNA, demethylation of nucleotides in DNA and RNA, and demethylation of LYSINE residues on certain proteins, including ACTIN and histones (HISTONE CODE).
Techniques for measuring specific nucleic acid interaction with another nucleic acid or with a protein by digestion of the non-interacting nucleic acid by various nucleases. After all non-interacting regions are eliminated by nuclease digestion, the protected nucleic acid that remains is analyzed. DNA FOOTPRINTING utilizes this technique to analyze the DNA contact sites of DNA-BINDING PROTEINS.
Double-stranded nucleic acid molecules (DNA-DNA or DNA-RNA) which contain regions of nucleotide mismatches (non-complementary). In vivo, these heteroduplexes can result from mutation or genetic recombination; in vitro, they are formed by nucleic acid hybridization. Electron microscopic analysis of the resulting heteroduplexes facilitates the mapping of regions of base sequence homology of nucleic acids.
Compounds that inhibit cell production of DNA or RNA.
A family of histone demethylases that share a conserved Jumonji C domain. The enzymes function via an iron-dependent dioxygenase mechanism that couples the conversion of 2-oxoglutarate to succinate to the hydroxylation of N-methyl groups.
Enzymes are proteins that catalyze (i.e., increase the rates of) chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical re...