Drug name: Temozolomide + 6-BG


Related CSCTT Targets

MGMT [ref.1]P16455

Temozolomide, Methazolastone

Cas.no PubChem ID
85622-93-1 5394
Known Target
DNA
Structure
...
Introduction
Temozolomide is an imidazotetrazine deritave and an antineoplastic agent. It is a prodrug that has little to no pharmacological activity until it is hydrolyzed in vivo to 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC). After administration, temozolomide undergoes rapid, nonenzymatic hydrolysis at physiological pH to MTIC, which is the active form of the drug. MTIC is generated through the effect of water at the highly electropositive C4 position of temozolomide, causing the ring of temozolomide to open, release carbon dioxide, and generate MTIC.

6-BG, 6-O-Benzylguanine

Cas.no PubChem ID
19916-73-5 4578
Known Target
Methylated-DNA--protein-cysteine methyltransferaseP16455
Structure
...
Introduction
O6-Benzylguanine (O6-BG) is a synthetic derivative of guanine. It is an antineoplastic agent. It exerts its effect by acting as an inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase which leads to interruption of DNA repair and increases the potency of other chemotherapeutic agents that damage DNA, such as temozolomide.

Reference

  • [1] Temozolomide preferentially depletes cancer stem cells in glioblastoma. Beier, D., et al. (2008).Cancer Res. 68(14):5706-15.
    18632623. [ 18632623 ]

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