| abstract |
(57) [Summary]nDisclosed are novel inhibitors of polyamine transport having an inhibition constant that is two orders of magnitude lower than that of known compounds. These polyamine analogs are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, such as cancer and post-angiogenic injury. A novel chemical synthesis method for obtaining polyamine analogs is disclosed, including the production of a combinatorial polyamine library. These approaches result in analogs having the desired activity in diagnostic and research assays and therapeutics. The assays of the invention are useful for high-throughput screening of targets in the discovery of drugs that interact with the polyamine system. |