The search textbox has an autosuggest feature. When you enter three or more characters, a list of up to 10 suggestions will popup under the textbox. Use the arrow keys to move through the suggestions. To select a suggestion, hit the enter key. Using the escape key closes the listbox and puts you back at the textbox. The radio buttons allow you to toggle between having all search items start with or contain the text you entered in the search box.
beta-lapachone prodrug ARQ 761
A synthetic, soluble prodrug of beta-lapachone, a poorly soluble, ortho-naphthoquinone with potential antineoplastic and radiosensitizing activity. ARQ 761 is converted to beta-lapachone (b-lap) in vivo. When b-lap is activated by NAD(P)H:quinone oxidoreductase-1 (NQO1) this agent creates a futile oxidoreduction, generating highly reactive oxygen species (ROS) that results in DNA damage. The activation of b-lap also causes hyperactivation of poly (ADP-ribose) polymerase-1 (PARP-1), an enzyme that facilitates DNA repair, accompanied by rapid depletion of NAD+/ATP nucleotide levels. As a result, a caspase-independent and endoplasmic reticulum (ER) stress-induced mu-calpain-mediated cell death occurs in NQO1-overexpressing tumor cells. In addition, b-lap induces expression of the checkpoints activator E2F transcription factor 1 (E2F1) and thereby activates the E2F1-mediated checkpoint pathway that directly triggers apoptosis. As ARQ 761 is soluble and requires less solvent, this formulation may cause less hemolytic anemia associated with administration of the synthetic b-lap ARQ 501. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
|Code name:||ARQ 761|