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.
AFP464
A synthetic lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and antineoplastic activities. AFP464 is rapidly converted to aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in cytochrome P450 1A1 (CYP1A1) and cytochrome P450 1A2 (CYP1A2) expression and, to a lesser extent, an increase in cytochrome P450 1B1 (CYP1B1) expression. Subsequently, aminoflavone is metabolized to toxic metabolites by the cytochromome P450 enzymes that it induces; these toxic metabolites covalently bind to DNA, resulting in the phosphorylation of p53, the induction of the p53 downstream target p21Waf1/Cip1, and apoptosis. Pulmonary toxicity may be dose-limiting. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)