Claims
- 1. A compound composed of 11-24 amino acid residues comprising the amino acid sequence:
- 2. The compound of claim 1 which comprises two disulfide bridges.
- 3. The compound of claim 2, wherein one of said disulfide bridges links C5-C16 and the other links C8-C13.
- 4. The compound of claim 3 which is selected from the group consisting of:
- 5. The compound of claim 2, wherein one of said disulfide bridges links C5-C8 and the other links C13-C16.
- 6. The compound of claim 5 which is selected from the group consisting of:
- 7. The compound of claim 2, wherein one of said disulfide bridges links C4-C17 and the other links C8-C13.
- 8. The compound of claim 7 which is selected from the group consisting of:
- 9. The compound of claim 1 which comprises one disulfide bridge.
- 10. The compound of claim 9 in which said disulfide bridge links C4-C17.
- 11. The compound of claim 10 which is selected from the group consisting of:
- 12. The compound of claim 9 in which said disulfide bridge links C5-C16.
- 13. The compound of claim 12 which is selected from the group consisting of:
- 14. The compound of claim 9 in which the disulfide bridge links C8 and C13.
- 15. The compound of claim 1 which is in the linear form.
- 16. The compound of claim 1 in which at least one of A1, A2 or A3 is not present.
- 17. The compound claim 1 in which A1, A2 and A3 are not present.
- 18. The compound of claim 1 in which at least one of A1, A2 or A3 is a hydrophobic amino acid.
- 19. The compound of claim 1 in which each of C5 and C16 is independently selected from the group consisting of cysteine, homocysteine, penicillamine, I, V, L, NLe, W, Y, F, A, S, G and T.
- 20. The compound of claim 1 in which each of C4 and C17 is independently selected from the group consisting of cysteine, homocysteine, penicillamine, I, V, L, NLe, W, Y, F, A, S, G and T.
- 21. The compound of claim 1 in which each of A7and A14 is independently selected from the group consisting of I, V, L, NLe, W, Y, F, A, S, G and T.
- 22. The compound of claim 1 in which one of A9 or A12 is R, K, Har, Orn or H and the other is I, V, L, NLe, W, Y, F, A, S, G or T.
- 23. The compound of claim 1 in which all amino acids are in the D-configuration.
- 24. The compound of claim 1 in which A7 and A14 are each independently a hydrophobic amino acid.
- 25. The compound of claim 1 in which A9 or A12 is a hydrophobic amino acid or a small amino acid.
- 26. The compound of claim 1 in which A10 and A11 are each independently selected from the group consisting of proline, a basic amino acid, a hydrophobic amino acid and a small amino acid.
- 27. The compound of claim 1 in which each of C8 and C13 is independently cysteine, homocysteine or penicillamine.
- 28. The compound of claim 1 in which A9-A10-A12 is selected from the group consisting of: R-R-R-F, R-G-W-I, R-P-R-F, X-R-R-F, R-X-RF, R-K-K-W, R-X-R-Y, R-R-K-W, r-R-R-F, R-x-R-F, R-G-R-F, C-R-G-R, Y-C-G-R, V-P-R-R-F, K-P-K-F, V-G-R-F, R-P-R-I and R-Z-R-F, where X is Har, x is D-Har, Z is MeGly and r is D-Arg.
- 29. The compound of claim 1 which is in the linear or disulfide-bridged form and which is selected from the group consisting of:
- 30. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable excipient.
- 31. A method of inhibiting the growth of a microbe or the replication of a virus which comprises the step of contacting said virus or said microbe with an amount of a compound according to claim 1 effective to inhibit said growth or said replication.
- 32. The method of claim 31 in which the microbe is a bacteria.
- 33. The method of claim 32 in which the bacteria is selected from the group consisting of E. coli, L. monocytogenes, B. subtilis, S. typhimurium, S. aureus and P. aeruginosa.
- 34. The method of claim 31 in which the microbe or virus is a sexually-transmitted microbe or virus.
- 35. The method of claim 34 in which the sexually-transmitted microbe or virus is selected from the group consisting of HIV-1, C. trachomatis, T. pallidum, N. gonorrhoeae, T. vaginalis, HSV-1, HSV-2, H. ducreyi and human papilloma virus.
- 36. The method of claim 31 in which the microbe or virus is HIV.
- 37. The method of claim 31 in which the microbe or virus is methicillin-resistant S. aureus (MRSA) or vancomycin-resistant E. faecalis (VREF).
- 38. A method to inactivate the endotoxin of gram-negative bacteria, which method comprises contacting said endotoxin with an amount of a compound according to claim 1 effective to inactivate said endotoxin.
- 39. A method to treat or prevent a microbial or viral infection in a subject, which method comprises administering to a subject in need of such treatment an amount of a compound according to claim 1 effective to ameliorate said infection in the subject.
- 40. The method of claim 39 in which the infection is a bacterial infection.
- 41. The method of claim 40 in which the bacteria is selected from the group consisting of E. Coli, L. monocytogenes, B. subtilis, S. typhimurium, S. aureus and P. aeruginosa.
- 42. The method of claim 39 in which the infection is caused by a sexually-transmitted pathogen.
- 43. The method of claim 42 in which the sexually-transmitted pathogen is selected from the group consisting of HIV-1, C. trachomatis, T. pallidum, N. gonorrhoeae, T. vaginalis, HSV-1, HSV-2, H. ducreyi and human papilloma virus.
- 44. The method of claim 39 in which the infection is an HIV infection.
- 45. The method of claim 39 in which the infection is a methicillin-resistant S. aureus (MRSA) or vancomycin-resistant E. faecalis (VREF) infection.
- 46. The method of claim 39 in which the compound is administered topically.
- 47. The method of claim 39 in which the compound is administered prophylactically.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation-in-part of application Ser. No. 08/674,622, filed Jul. 3, 1996, which is a continuation-in-part of provisional application Ser. No. 60/000,898, filed Jul. 6, 1995. The contents of these applications are hereby incorporated herein by references in their entireties.
Government Interests
[0002] This invention was made with funding from NIH Grant No. A122839. The U.S. Government has certain rights in this invention.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60000898 |
Jul 1995 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09128344 |
Aug 1998 |
US |
Child |
09865943 |
May 2001 |
US |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
08674622 |
Jul 1996 |
US |
Child |
09128344 |
Aug 1998 |
US |