G-quadruplex binding assays and compounds therefor

Abstract

The present invention provides methods for assaying binding of compounds to G-quadruplex structures. Also provided are methods for screening candidate compounds for use as modulators of G-quadruplex activity, and methods for screening candidate compounds for telomerase inhibitory activity. The invention further provides novel compounds useful in the assays of the invention.

What is claimed is: 
     
         1 . A compound comprising any of SEQ ID NOs: 2-8 wherein at least one G nucleobase therein has been replaced with a 6-methyl-isoxanthopterin nucleobase, provided that said compound forms a G-quadruplex structure;
 wherein each 6-methyl-isoxanthopterin nucleobase is located within said G-quadruplex structure;   and  6 -methyl-isoxanthopterin nucleobase replaces the G nucleobase at position 11 of either of SEQ ID nos 2-3, one or more of the G nucleobases at positions 11 or 23 of either of SEQ ID NOs: 4-5; one or more of the G nucleobases at positions 11, 23, or 35 of either of SEQ ID NOs: 6-7, or one or more of the G nucleobases at positions 11, 23, 35, or 47 of SEQ ID NO. 8.   
     
     
         2 . The compound of  claim 1 , wherein said compound contains one 6-methyl-isoxanthopterin nucleobase. 
     
     
         3 . The compound of  claim 1 , wherein said compound contains two 6-methyl-isoxanthopterin nucleobases. 
     
     
         4 . The compound of  claim 1 , wherein the compound comprises any of SEQ ID NOs: 2-8. 
     
     
         5 . The compound of  claim 1 , wherein the compound comprises any of SEQ ID NOs: 3-5. 
     
     
         6 . The compound of  claim 1 , wherein the compound comprises SEQ ID NO: 4. 
     
     
         7 . An array comprising the compound of  claim 1 . 
     
     
         8 . An array comprising the compound of  claim 2 .