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.

1 . (canceled) 
     
     
         2 . A compound comprising any of SEQ ID NOs: 1-8 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 wherein each of said 6-methyl-isoxanthopterin nucleobases are located at one or more of the G5 or G11 positions thereof.   
     
     
         3 . The compound of  claim 2 , wherein said compound contains one 6-methyl-isoxanthopterin nucleobase. 
     
     
         4 . The compound of  claim 2 , wherein said compound contains two 6-methyl-isoxanthopterin nucleobases. 
     
     
         5 . The compound of  claim 2 , wherein the compound comprises any of SEQ ID NOs: 2-8. 
     
     
         6 . The compound of  claim 2 , wherein the compound comprises any of SEQ ID NOs: 3-5. 
     
     
         7 . The compound of  claim 2 , wherein the compound comprises SEQ ID NO: 4. 
     
     
         8 . An array comprising the G-quadruplex analog polynucleotide of  claim 2 . 
     
     
         9 . An array comprising the G-quadruplex analog polynucleotide of  claim 3 .