The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 10, 1998

Filed:

Apr. 24, 1995
Applicant:
Inventors:

Gordon R Julian, Bozeman, MT (US);

Jesse M Jaynes, Raleigh, NC (US);

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07K / ; C07K / ; C07K / ; A61K / ;
U.S. Cl.
CPC ...
530324 ; 514 12 ;
Abstract

A tryptic digestion-resistant, non-naturally occurring lytic peptide comprising a sequence of amino acid residues containing mainly alanine, valine and lysine amino acid residues, wherein the .epsilon.-amino groups of the lysine residues and the .alpha.-amino group of the N-terminal amino acid are sufficiently methylated to impart enhanced tryptic, chymotryptic, and aminopeptidase digestion resistance to the peptide. The secondary conformation of the peptide is an ordered periodic structure such as an amphipathic .alpha.-helix or a .beta.-pleated sheet. The compositions of the invention are suitable for in vivo administration. A method of making the same, to impart enhanced tryptic digestion-resistance thereto, comprising reductively alkylating the .epsilon.-amino groups of the lysine residues and the .alpha.-amino group of the N-terminal amino acid with a methyl-providing reagent in the presence of an heterocyclic amine-borane reducing agent for sufficient time and at sufficient conditions to methylate the .alpha.-and .epsilon.-amino groups to sufficient extent to confer enhanced proteolytic digestion-resistance to the peptide.


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