Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 15 to 23 amino acid residues in defined sequence
Patent
1997-10-06
1998-08-04
Tsang, Cecilia J.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
15 to 23 amino acid residues in defined sequence
514 14, 435259, C07K 708, C12N 106
Patent
active
057895422
ABSTRACT:
Minimalist lytic peptides are disclosed that may be readily synthesized on a large scale via a highly-convergent, solution-phase synthesis. The peptides are amphipathic, and are easy and inexpensive to synthesize via solution phase techniques. The peptides exhibit anti-bacterial properties at concentrations that are not lethal to normal mammalian cells. The peptides comprise multimers, i.e. two or more repeats, of certain heptads of amino acid residues. The heptads were designed to generate amphipathic peptides when the heptads are combined into multimers, and were further designed to be readily suited for convergent, solution-phase synthesis. The preferred heptads are described generically by one of the following four formulas, in which "Xps" denotes a positively charged amino acid at physiological pH, and in which "Xnp" denotes a nonpolar amino acid at physiological pH: (1) Xps.sub.1 Xnp.sub.1 Xnp.sub.2 Xps .sub.1 Xnp.sub.1 Xnp.sub.2 Xps, or (2) XpsXnp.sub.1 Xnp.sub.2 Xps.sub.1 Xnp.sub.1 Xnp.sub.2 Xps.sub.1, or (3) Xps.sub.1 Xnp.sub.1 Xnp.sub.2 XpsXps.sub.1 Xnp.sub.1 Xnp.sub.2, or (4) XpsXps.sub.1 Xnp.sub.1 Xnp.sub.2 Xps.sub.1 Xnp.sub.1 Xnp.sub.2. Other heptads are also disclosed.
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Becker Calvin L.
McLaughlin Mark L.
Board of Supervisors of Louisiana State University and Agricultu
Gupta Anish
Runnels John H.
Tsang Cecilia J.
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