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Antisense EGFRAS guanidinium peptide nucleic acid (GPNA) oligonucleotides as antitumor agents
US9334496B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9334496-B2 |
| Application number | US-201113107344-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 13, 2011 |
| Priority date | Nov 13, 2006 |
| Publication date | May 10, 2016 |
| Grant date | May 10, 2016 |
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Abstract
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A class of antisense agents having a distributed guanidinium peptide nucleic acids (GPNA) backbone which has excellent uptake into mammalian cells, can bind to the target DNA or RNA in a highly sequence specific manner and can resist nucleases and proteases both outside and inside the cell(s) of interest. In one embodiment, either systemic or intratumoral administration of antisense Epidermal Growth Factor Receptor (“EGFR”) GPNA oligonucleotides is believed to downmodulate EGFR levels, thus in turn to reduce head and neck squamous cell carcinoma tumor growth, which has been confirmed to date both in vitro and in vivo.
First claim
Opening claim text (preview).
The invention claimed is: 1. A method for the treatment of malignancy comprising administering systemically or intratumorally an antisense oligonucleotide comprising at least one peptide nucleic acid “PNA”, the peptide nucleic acid comprising a guanidinium peptide (GPNA), to a patient in need of such treatment, further wherein said oligonucleotide consists of a GPNA based on EGFR mRNA wherein said GPNA has both unmodified PNA and four or more arginine-derived GPNA substitutions. 2. A peptide nucleic acid “PNA” selected from the group consisting of 5′-A R GC R AG R CT R CCCA R TT R GG R G-3′ (SEQ ID NO:1) or 5′-AG R CA R GC R TC R CC R AT R TG R GG-3′ (SEQ ID NO:7), where the subscript R denotes an arginine-derived guanidinium peptide nucleic acid substitution.
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Classifications
Peptide nucleic acid, PNA · CPC title
modulating the chemical stability, e.g. nuclease-resistance · CPC title
Antisense · CPC title
against receptors or cell surface proteins · CPC title
- C12N15/111Primary
General methods applicable to biologically active non-coding nucleic acids · CPC title
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- What does patent US9334496B2 cover?
- A class of antisense agents having a distributed guanidinium peptide nucleic acids (GPNA) backbone which has excellent uptake into mammalian cells, can bind to the target DNA or RNA in a highly sequence specific manner and can resist nucleases and proteases both outside and inside the cell(s) of interest. In one embodiment, either systemic or intratumoral administration of antisense Epidermal G…
- Who is the assignee on this patent?
- Grandis Jennifer Rubin, Thomas Sufi Mary, Ly Danith H, and 3 more
- What technology area does this patent fall under?
- Primary CPC classification C12N15/111. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue May 10 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).