Synthetic triplex peptide nucleic acid-based inhibitors for cancer therapy
AssigneeUniversity of Connecticut
InventorsRaman Bahal, Shipra Malik, Vikas Kumar
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Abstract
A novel peptide nucleic acid (PNA) oligomer capable of forming a PNA/DNA/PNA triplex when binding to its target genomic DNA is described. An PNA oligomer directed to C-Myc oncogene was capable of binding the target DNA and effectively inhibit the transcription of the gene both in vitro as well as in vivo without causing any toxicity. Methods of making and using the novel PNA oligomer for targeting other genomic DNA are described.
Claims20
A peptide nucleic acid analogue (PNA) oligomer that forms a PNA/DNA/PNA triplex invasion complex with a homopurine region of a target deoxyribonucleic acid (DNA), wherein the PNA oligomer has the formula:
- 5′-first PNA segment-flexible linker 1-second PNA segment-3′
- wherein
- the first PNA segment is complementary to a homopurine stretch in the target DNA,
- the second PNA segment is complementary to a region of the target DNA including the homopurine stretch,
- a nuclear localization signal (NLS) peptide is conjugated to a carboxyl-terminus (C-terminus), an amino-terminus (N-terminus), or both the C-terminus and N-terminus of the PNA oligomer,
- the first PNA segment and the second PNA segment form the PNA/DNA/PNA triplex structure with the target DNA, and
- the target DNA is genomic DNA.
Dependencies are inferred from the claim text.