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.
Patent No.:
Date of Patent:
Jun. 22, 1993
Filed:
Dec. 06, 1988
Hao-Chia Chen, Potomac, MD (US);
Judith H Brown, Falls Church, VA (US);
John L Morell, Bethesda, MD (US);
Charng-Ming Huang, Bethesda, MD (US);
Abstract
Peptides which exhibit improved broad spectrum antimicrobial activity are designed and synthesized based on the peptide sequences of magainin or PGS peptides. The modified peptide analogues are synthesized by replacing low helical potential amino acid residues with high helical potential residues and modifying the two termini in order to enhance the amphiphilic structures as well as to prolong antimicrobial activity by lowering their susceptibility to protease degradation. For example, low propensity residues within a strategic region of magainin II, e.g. Ser.sup.8, Gly.sup.13 and Gly.sup.18 are modified with Ala which is known to have high propensity. Amidation of Ser.sup.23, and acylation of Gly.sup.1 with acetyl or beta-alanyl and substitution of Gly.sup.1 with beta-alanine are carried out in order to lower the susceptibility to exopeptidase action. A D-Ala modification for disrupting a stretch of the helical structure is also prepared so as to demonstrate the importance of an amphiphilic helical structure for antimicrobial activity. The modified peptide analogues exhibit an increase of up to two orders of magnitude in antimicrobial activity and, in the most favorable case, no appreciable increase in hemolytic activity over magainin 1.