Amphipathic peptides
US5789542A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Oct 6, 1997 |
| Grant date | Aug 4, 1998 |
| Priority date | — |
| Expiry date | Oct 6, 2017 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.