Stereochemical control of the DNA binding affinity, sequence specificity, and orientation-preference of chiral hairpin polyamides in the minor groove
US7049061B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 12, 1999 |
| Grant date | May 23, 2006 |
| Priority date | — |
| Expiry date | Aug 12, 2019 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention provides improved polyamides comprising a hairpin loop derived from γ-aminobutyric acid which bind to the minor groove of a promoter regions of a DNA sequence. Binding of the polyamide to the DNA sequence of the promoter region inhibits expression of the requisite gene. The improvement relates to the use of R-2,4-diaminobutyric acid and derivatives of the 2-amino group to form the hairpin loop. The improved asymmetric hairpin provides for tighter binding of the polyamides to the minor groove of DNA and additionally provides an amine function for derivatizing polyamides by, for example, forming amide linkages. Such derivatives may serve to attach detectable labels to the polyamide.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.