Lipid conjugates of therapeutic peptides and protease inhibitors

Details Lipid conjugates of therapeutic peptides and protease inhibitors Lipid conjugates of therapeutic peptides and protease inhibitors

1991-07-23

1996-09-10

Scheiner, Toni R.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

11 to 14 amino acid residues in defined sequence

530328, 530329, 530330, 530331, 530345, 548535, 562561, C07K 500, C07K 700, C07K 1700, A61K 3800

Patent

active

055547281

ABSTRACT:
Compounds wherein therapeutic peptides are covalently linked to phospholipids, glycerides or other membrane-targeting and membrane-anchoring species, and their pharmaceutically acceptable salts, together with processes for their preparation. The targeting technology is applicable to HIV protease inhibitors and a variety of other enzyme inhibitors.

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patent: 5411947 (1995-05-01), Hostetler et al.
Biochemical and Biophysical Research Communications, vol. 156, No. 1, issued Oct. 14, 1988, Darke et al., "HIV-1, protease specificity of peptide cleavage is sufficient for processing of GAG and POL polyproteins" pp. 297-303.
Merrifield, R., Solid-Phase Peptide Synthesis, J. Chem. Soc. 85:2149 (1963).
Blaug, S., Remington's Pharmaceutical Sciences 15th Ed.: Chapter 87 (1975).
Dreyer, G., et al., Inhibition of human immunodeficiency virus 1 protease in vitro . . . Proc. Nat'l. Acad. Sci. USA 86:9752-9756 (1989).
Meek, T. et al., Inhibition of HIV protease in infected T-lymphocites by synthetic peptide analogues. Nature 343:90-92 (1990).
McQuade, T. et al, A Synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation. Science 247:454-456 (1990).
Wlodawer, A., et al., Conserved Folding in Retroviral Proteases: Crystal Structure . . . Research Articles 245:616-621 (1989).
Marx, Jean L., NCI Team Remodels Key AIDS Virus Enzyme. Science 245:598 (1989).
Blundell, T. and Pearl, L., A second front against AIDS. Nature 337:596-597 (1989).

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