Literature summary for 1.6.5.2 extracted from

Sasaki, J.; Sano, K.; Hagimori, M.; Yoshikawa, M.; Maeda, M.; Mukai, T.
Synthesis and in vitro evaluation of radioiodinated indolequinones targeting NAD(P)H quinone oxidoreductase 1 for internal radiation therapy (2014), Bioorg. Med. Chem., 22, 6039-6046 .

Search for more literature for 1.6.5.2

Application

Application	Comment	Organism
medicine	development of an NQO1-targeted radiolabeled agent to establish an internal radiation therapy that amplifies the therapeutic effects when combined with external radiation therapy. The uptake of [125I]-marked compound 3-([[4-iodophenyl]thio]methyl)-5-methoxy-1,2-dimethyl-1H-indole-4,7-dione is specific and is dependent on the expression of NQO1. In NQO1-expressing tumor cells, over 85% of the initial radioactivity of [125I]-marked 3-([[4-iodophenyl]thio]methyl)-5-methoxy-1,2-dimethyl-1H-indole-4,7-dione is observed as an intact form at 1 h after incubation	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
3-([[4-Iodophenyl]thio]methyl)-5-methoxy-1,2-dimethyl-1H-indole-4,7-dione	compound based on the selective binding of indolequinone analogs to the active site of NQO1 by the stacking effect. [125]I-marked compound can be used as an internal radiation agent for the treatment of cancer	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P15559	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HT-29 cell	-	Homo sapiens	-

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)