Antisense guanidinium peptide nucleic acid (GPNA)...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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Reexamination Certificate

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07960360

ABSTRACT:
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.

REFERENCES:
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patent: 2002/0155989 (2002-10-01), Efimov et al.
patent: 2005/0107325 (2005-05-01), Manoharan et al.
patent: 2007/0072802 (2007-03-01), Zhao et al.
Escude et al. (Top. Curr. Chem 253:109-148, 2005).
Zhou et al. (J. Am. Chem. Soc. 125:6878-6879, 2003).
Dragulescu-Andrasi et al., “Cell-permeable GPNA with appropriate backbone stereochemistry . . . ,” Chem. Commun., 2005, pp. 244-246.
Wender, P. et al., “The design, synthesis, and evaluation of molecules . . . ” PNAS, vol. 97, No. 24, pp. 13003-13008, Nov. 21, 2000.

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