Antisense EGFRAS guanidinium peptide nucleic acid (GPNA) oligonucleotides as antitumor agents

US9334496B2 · kind B2 · utility

Assignees

• EYE & EAR FOUNDATION · US
• University of Pittsburgh—Of the Commonwealth System of Higher Education · US
• CARNEGIE MELLON UNIVERSITY · US

Inventors

• Jennifer Rubin Grandis · Pittsburgh, US
• Sufi Mary Thomas · Springdale Township, US
• Danith H. Ly · Pittsburgh, US

Key dates

• Filing date: May 13, 2011
• Grant date: May 10, 2016
• Expiry date: May 13, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12N2320/51
• WIPO field: Biotechnology
• WIPO sector: Chemistry

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.