Viral integrase inhibiting peptides

Details Viral integrase inhibiting peptides Viral integrase inhibiting peptides

1995-01-20

1996-11-26

Russel, Jeffrey E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

435194, 530329, A61K 3808, C07K 706, C12N 912

Patent

active

055785735

ABSTRACT:
The present invention provides viral integrase inhibiting peptides having the general structure, ##STR1## where Xaa is an amino acid or an amino acid analog, the stereochemistry of the amino acids or amino acid analogs can be D-amino acids or L-amino acids and the amino and carboxy termini of the peptide can be modified. The invention also provides viral inhibiting peptides having essentially the amino acid sequence, ##STR2## The invention also provides a pharmaceutical composition comprising a viral integrase inhibiting peptide and methods of using a viral integrase inhibiting peptide in vitro or in vivo to reduce or inhibit viral integrase activity in a cell and the infectivity of a virus.

REFERENCES:
patent: 5141735 (1992-08-01), Bellemin et al.
patent: 5413914 (1995-05-01), Franzusoff
Neuzil, Kathleen Maletic, "Pharmacologic Therapy for Human Immunodeficiency Virus Infection: A Review." Amer. J. Med. Sci. 307:368-373 (1994).
Cushman and Sherman, "Inhibition of HIV-1 Integration Protein by Aurintricarboxylic Acid Monomers, Monomer Analogs, and Polymer Fractions." Biomed. Biophy. Res. Comm. 185:85-90 (1992).
Fesen, Mark R. et al., "Inhibitors of Human Immunodeficiency Virus Integrase." Proc. Natl. Acad. Sci. USA 90:2399-2403 (1993).
Fesen, Mark R. et al., "Inhibition of HIV-1 Integrase by Flavones, Caffeic Acid Phenethly Ester (CAPE) and Related Compounds." Biomed. Pharm. 48:595-608 (1994).
Lafemina, Robert L. et al., "Inhibition of Human Immunodeficiency Virus Integrase by Bis-Chatechols." Antimicr. Agents. and Chemother. 39:320-324 (1995).
Mazumder, Abhijit et al., "Inhibition of Human Immunodeficiency Virus Type 1 Integrase by 3'-azido-3'-deoxythymidylate." Proc. Natl. Acad. Sci. USA 91:5771-5775 (1994).
Mazumder, Abhijit et al., "Inhibition of Human Immunodeficiency Virus Type 1 Integrase by a Hydrophobic Cation: The Phenanthroline-Cuprous Complex." Aids Res. and Human Retro. 11:115-125 (1995).

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