EXPONENTIAL PATTERN RECOGNITION BASED CELLULAR TARGETING, COMPOSITIONS, METHODS AND ANTICANCER APPLICATIONS

摘要

The present invention relates to the compositions, methods, and applicationsof a new approach to pattern recognition based targeting by which anexponential amplification of effector response can be specifically obtained ata targeted cells. The purpose of this invention is to enable the selectivedelivery of large quantities of an array of effector molecules to target cellsfor diagnostic or therapeutic purposes. The invention is comprised of twocomponents designated as "Compound 1" and "Compound 2": Compound 1 iscomprised of a cell binding agent and a masked female adaptor. Compound 2 iscomprised of a male ligand, an effector agent, and two or more masked femalereceptors. The male ligand is selected to bind with high affinity to thefemale adaptor. Compound 1 can bind with high affinity to the target cell andthe female receptor can then be unmasked by an enzyme enriched at the tumorcell. The male ligand of Compound 2 can then bind to the unmasked femaleadaptor bound to the target cell. The masked female adaptor on the boundCompound 2 can then be specifically unmasked. One receptor has in effectbecome two. Two new molecules of Compound 2 can bind to the unmasked adaptorsreceptors. After unmasking two receptors in effect become four. The processcan continue in an explosive exponential like fashion resulting in enormousamplification of the number of effector molecules specifically deposited atthe target cell.