Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors.
N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays.
Hamada
Shohei
S
Nagoya City University, Tanabe-dori, Mizuho-ku, Aichi, Japan.
Kim
Tae-Dong
TD
Suzuki
Takayoshi
T
Itoh
Yukihiro
Y
Tsumoto
Hiroki
H
Nakagawa
Hidehiko
H
Janknecht
Ralf
R
Miyata
Naoki
N
D000600:Amino Acids, Dicarboxylic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D056484:Jumonji Domain-Containing Histone Demethylases; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010089:Oxidoreductases, N-Demethylating / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000600:Amino Acids, Dicarboxylic; D004791:Enzyme Inhibitors; C413655:KDM4C protein, human; D009363:Neoplasm Proteins; D014157:Transcription Factors; D056484:Jumonji Domain-Containing Histone Demethylases; C521694:KDM4D protein, human; C494424:KDM4A protein, human; D010089:Oxidoreductases, N-Demethylating; C040947:oxalylglycine