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US 6,307,016 B1Granted
Parevins and tachytegrins
AssigneeIntraBiotics Pharmaceuticals, Inc.
InventorsRobert I. Lehrer, Sylvia S. L. Harwig, Conway C. Chang, Chee L. Gu
Life of this patent
Estimating the term…
Abstract
The present invention provides a new class of broad-spectrum antimicrobial peptides effective against a wide variety of microbes, including bacteria, viruses, retroviruses, fungi, yeast and protozoa.
Claims22
An antimicrobial compound composed of 11-24 amino acid residues comprising the amino acid sequence:
- A1-A2-A3-C4-C5-C6-A7-C8-A9-A10-A11-A12-C13-A14-C15-C16-C17-A18
- or a pharmaceutically acceptable salt or an N-terminal acylated or C-terminal amidated or esterified form thereof, wherein:
- each of A1-A3 is independently present or not present, and if present each is independently a basic, hydrophobic, polar/large, or small amino acid;
- each of C4 and C17 is independently present or not present, and if present each is independently selected from the group consisting of a thiol-containing amino acid, a basic amino acid, a hydrophobic amino acid, a polar/large amino acid and a small amino acid;
- C5 is selected from the group consisting of a thiol-containing amino acid, a basic amino acid, a hydrophobic amino acid, a polar/large amino acid and a small amino acid;
- each of C8 and C13 is independently a thiol-containing amino acid;
- each of C6and C15 is independently selected from the group consisting of a thiol-containing amino acid, a basic amino acid, a hydrophobic amino acid, a polar/large amino acid, a small amino acid and an acidic amino acid;
- C16 is selected from the group consisting of a thiol-containing amino acid, a hydrophobic amino acid or a small amino acid;
- each of A7 and A14 is independently a hydrophobic or a small amino acid;
- A9-A12 taken together are capable of effecting a β-turn when contained in the compound and at least one of A9-A12 is a basic amino acid;
- A18 is present or not present, and if present, is a basic, hydrophobic, polar/large, or small amino acid;
- at least about 15% to about 50% of the amino acid residues composing said compound are basic amino acids;
- and
- said compound has a net positive charge of at least +1 at physiological pH;
- with the provisos that:
- (i) when one of C4, C5 or C6 is a thiol-containing amino acid, the other two are other than a thiol-containing amino acid;
- (ii) when one of C15, C16 or C17 is a thiol-containing amino acid, the other two are other than a thiol-containing amino acid;
- and (iii) the compound has one feature selected from the group consisting of:
- (1) C4 and C15 are each independently a thiol-containing amino acid;
- (2) C4 and C16 are each independently a thiol-containing amino acid;
- (3) C4 and C17 are each independently a thiol-containing amino acid;
- (4) C5 and C15 are each independently a thiol-containing amino acid;
- (5) C5 and C16 are each independently a thiol-containing amino acid;
- (6) C6 and C16 are each independently a thiol-containing amino acid;
- and
- (7) C6 and C17 are each independently a thiol-containing amino acid.
23 more elements
Dependencies are inferred from the claim text.