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.
Nagoya City University, Tanabe-dori, Mizuho-ku, Aichi, Japan.
Shohei
S
Hamada
Tae-Dong
TD
Kim
Takayoshi
T
Suzuki
Yukihiro
Y
Itoh
Hiroki
H
Tsumoto
Hidehiko
H
Nakagawa
Ralf
R
Janknecht
Naoki
N
Miyata
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