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DI 01-13, 02-57 and 02-84

Novel targeting peptides for intracellular
delivery of compounds:
research and therapeutic applications

Inventor: Alphonse GARCIA et al.

Description of invention:

Intracellular delivery of small molecules, oligonucleotides and functionally active peptides across biological membranes represents a challenge to researchers developing new therapeutic strategies against cancer, infectious diseases, and other illnesses. Various scientific teams worldwide have focused on identifying novel peptides capable of penetrating cellular membranes, carrying substances of interest and targeting to specific cell components, particularly the nucleus, but also the cytoplasma.

In the present invention, researchers at the Institut Pasteur have designed short (12-20 amino acids) peptide sequences based on their ability to interact with protein phosphatase 2A (PP2A). Some of these peptides were found to cross the cell membrane in eukaryotes and were able to target molecules to the cytosol and/or the nucleus. These peptides are nontoxic and can be used to generate intracellular-targeting tools such as expression vectors. In addition, they can be coupled with other peptides, DNA molecules or other substances to allow effective delivery of these molecules into cells. These peptides could serve as in vitro and in vivo delivery devices for delivery of small molecules to cells.

Potential applications and advantages:

Carry pharmacologically active compounds into infected cells in therapeutic applications

Deliver inhibitory peptides into cell cytoplasm and nucleus to control physiological processes, block nuclear receptors
Disrupt gene activity when linked to antisense oligonucleotides or nucleic acids
Research tool for in vivo studies, combined with microinjection technology.
More effectively target therapeutic compounds to intracellular parasites such as T. gondii, Leishmania, P. falciparum, as well as bacteria such as Chlamydia and Listeria.

Patent Status:

French patent application filed July 27, 2001; PCT application published on Feb. 13, 2003 as WO 03011898
second French patent application filed January 29, 2003

Contact : Christophe Poquet, Business Development Manager - Office of Technology Transfer
 Institut Pasteur - 28 Rue du Docteur Roux - 75724 Paris Cedex 15 FRANCE
Tel : 33.(0)1.40 61 33 97 - Fax : 33.(0) - email :