DNA Binding Compounds for Genetic Regulation and Medical Diagnosis and Therapy

Compounds that bind to DNA could be used to target drugs to DNA and to regulate expression of genes. Indeed, many compounds have been discovered (e.g. Distamycin) which bind to the minor groove of DNA, but the bond is too weak for reliable medical application.

Scientists at the University of California have discovered a class of novel compounds that have a high binding affinity for DNA (Keq>=109 M-1). The compounds bind in the minor grooves of the double helix and extend into the major groove to a substituent which interacts strongly in the major groove, particularly at the phosphodiester linkages. The side groups of the compounds also may bind metal ions.

These novel compounds have multiple therapeutic and diagnostic applications. The compounds inhibit mammalian topoisomerase, a molecule that unwinds and rewinds the DNA double helix during replication. They function by competing for binding sites, altering the conformation of the DNA, and changing the affinity of DNA manipulating enzymes for sites on the double helix. Further, these compounds could be effective to arrest cell growth and act as anti-cancer agents. Since these compounds detect nucleic acid with high sensitivity, they may be used for diagnostic purposes. For instance, they may be used to assay for the presence of DNA or RNA markers of a disease in a sample of infectious material. Protein, mass produced by recombinant DNA technology, may be checked for the presence of minute quantities of DNA or RNA.

For therapeutic treatments, the compounds may be combined with pharmaceutical carriers and made into a liquid, tablet, powder, suppository, or ointment. Besides oral or topical application of the dose, the compounds may be introduced intravenously or by injection directly into the peritoneal cavity, lymphatic system, or malignant tumors.

REFERENCE: 1993-115

US 5,698,674   [MORE INFO]

Type of Offer: Licensing

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