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Retro-Inversion Peptides That Target GIT Transport Receptors and Related Methods

a technology of git transport receptor and retroinversion peptide, which is applied in the field of peptides, can solve the problems of peptides susceptible to degradation in the git, and achieve the effects of enhancing active agent delivery, promoting uptake of active agents, and enhancing the stability of proteases

Inactive Publication Date: 2009-09-24
MERRION RES III LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Proteases cleave peptide bonds between adjacent L-amino acids, rendering these peptides susceptible to degradation in the GIT.

Method used

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  • Retro-Inversion Peptides That Target GIT Transport Receptors and Related Methods
  • Retro-Inversion Peptides That Target GIT Transport Receptors and Related Methods
  • Retro-Inversion Peptides That Target GIT Transport Receptors and Related Methods

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Embodiment Construction

[0008]The present invention relates to retro-inverted peptides (also referred to herein as “targeting retro-inverted peptides” or “targeting retro-inversion peptides”) that target specific receptor sites in vivo and / or promote uptake of active agents and / or enhance active agent delivery across the GIT into the systemic, portal or hepatic circulation. In particular, these retro-inverted peptides specifically bind to one or more of the human gastro-intestinal tract receptors HPT1, HPEPT1, D2H or hSI or their equivalents in other mammals and have general utility in targeting active agents to selected sites and / or selected tissues in the body in which the receptors are expressed. These peptides are synthesized from D-amino acids and have a reverse sequence order of the GIT targeting agents disclosed and claimed in the above-referenced WO 98 / 51325. The present invention also relates to derivatives (including but not limited to fragments) of these retro-inverted peptides, which derivative...

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Abstract

Retro-inverted forms of GIT targeting agents that target specific receptor sites in vivo and / or promote uptake of active agents and / or enhance active site delivery across the GIT into the systemic circulation are provided. These retro-inverted peptides and compositions containing these retro-inverted peptides can be used to deliver an active agent, such as a drug or a drug-containing nano- or microparticle for treatment of a condition in a subject in need of the drug, in vivo. Additionally, the invention provides antibodies which are capable of immunospecifically binding the retro-inverted peptides.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation application of U.S. application Ser. No. 09 / 443,986, filed Nov. 19, 1999, allowed, which claims the benefit of U.S. Provisional Application Ser. No. 60 / 109,038, filed Nov. 19, 1998, which applications are incorporated by reference herein in their entireties.FIELD OF THE INVENTION[0002]The present invention relates generally to peptides that are capable of targeting or specifically binding gastro-intestinal tract (GIT) transport receptors. In particular, the invention relates to retro-inverted forms of peptide sequences and motifs, as well as derivatives thereof, which enhance drug delivery and transport through tissue, such as epithelial cells lining the luminal side of the GIT. Production of peptides and antibodies is also provided. The invention further relates to pharmaceutical compositions, formulations and related methods.BACKGROUND OF THE INVENTION[0003]Proteases cleave peptide bonds between adjace...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/16C07K19/00A61K38/28A61K38/16A61K9/14A61K38/00A61K45/00A61K47/48A61P3/10A61P9/00A61P9/04A61P9/12A61P19/10A61P25/06A61P35/00C07K7/02C07K7/08C07K14/00C07K16/44
CPCA61K38/00C07K7/02A61K47/48276A61K47/6425A61P19/10A61P25/06A61P35/00A61P9/00A61P9/04A61P9/12A61P3/10
Inventor O'MAHONY, DANIEL JOSEPH
Owner MERRION RES III LTD