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Method and composition for enhancing transport across biological membranes

  • US 6,495,663 B1
  • Filed: 09/14/1999
  • Issued: 12/17/2002
  • Est. Priority Date: 05/21/1997
  • Status: Expired due to Term
First Claim
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1. A conjugate for administration, to a mammalian subject, of an antimicrobial agent whose efficacy in non-conjugated form is limited by its solubility in aqueous liquid or its inability to cross biological membranes to manifest biological activity, said conjugate comprises a transport peptide covalently attached by a linker to the antimicrobial agent, said linker being cleaved in vivo to release the antimicrobial agent from the linker and the transport peptide, wherein the attached transport peptide:

  • (a) consists of from 6 to 25 amino acid residues, at least 50% of which contain a guanidino sidechain having the structure embedded imageor an amidino sidechain having the structure embedded imagewherein n is 2, 3, 4 or 5;

    (b) contains at least 6 contiguous amino acid residues containing said guanidino or amidino sidechain; and

    (c) increases the delivery of the antimicrobial agent across a biological membrane relative to the delivery of the antimicrobial agent in non-conjugated form.

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