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Details for Patent: 6,824,783

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Details for Patent: 6,824,783

Title: Methods for inhibition of membrane fusion-associated events, including HIV transmission
Abstract:The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1.sub.LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.
Inventor(s): Bolognesi; Dani Paul (Durham, NC), Matthews; Thomas James (Durham, NC), Wild; Carl T. (Durham, NC)
Assignee: Duke University (Durham, NC)
Filing Date:Jun 07, 1995
Application Number:08/487,266
Claims:1. A method for the inhibition of transmission of HIV-1 to a cell, comprising contacting the virus, in the presence of the cell, with an effective concentration of a peptide for an effective period of time, so that infection of the cell by the virus is inhibited, wherein the peptide has the formula:

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

2. The method of claim 1, wherein X is an acetyl group, and Z is an amido group.

3. The method of claim 1, wherein X is an amino group.

4. The method of claim 1, wherein Z is a carboxyl group.

5. The method of claim 1, wherein X is a 9-fluorenylmethoxy-carbonyl group.

6. A method for inhibiting HIV-1 infection of a cell, comprising contacting the virus, in the presence of the cell, for an effective period of time with an effective amount of a peptide having the formula:

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

7. A method for treating or delaying the onset of AIDS in an HIV-1 infected individual, comprising administering to the individual an effective amount of a peptide having the formula:

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

8. A method for increasing the number of CD4.sup.- cells in an HIV-1 infected individual, comprising administering to the individual an effective amount of a peptide having the formula:

X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ ID NO:1);

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

9. A method for lowering plasma levels of HIV-1 in an individual, comprising administering to the individual an effective amount of a peptide having the formula:

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

10. The method of claim 6, wherein X is a hydrophobic group.

11. The method of claim 10, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

12. The method of claim 6, wherein Z is a hydrophobic group.

13. The method of claim 12, wherein the hydrophobic group Z is t-butyloxycarbonyl.

14. The method of claim 6, wherein X is a macromolecular carrier group.

15. The method of claim 14, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

16. The method of claim 6, wherein Z is a macromolecular carrier group.

17. The method of claim 16, wherein the macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

18. The method of claim 6, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

19. The method of claim 18, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

20. The method of claim 6, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

21. The method of claim 6, wherein X is an acetyl group, and Z is an amido group.

22. The method of claim 14, wherein the macromolecular carrier group X is a peptide group.

23. The method of claim 16, wherein the macromolecular carrier group Z is a peptide group.

24. The method of claim 23, wherein X is a peptide macromolecular carrier group and Z is a peptide macromolecular carrier group.

25. The method of claim 6, wherein X is an amino group.

26. The method of claim 6, wherein Z is a carboxyl group.

27. The method of claim 6, wherein X is a 9-fluorenylmethoxy-carbonyl group.

28. The method of claim 6, further comprising contacting the virus with a pharmaceutically acceptable carrier.

29. The method of claim 7, wherein X is a hydrophobic group.

30. The method of claim 29, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

31. The method of claim 7, wherein Z is a hydrophobic group.

32. The method of claim 31, wherein the hydrophobic group Z is t-butyloxycarbonyl.

33. The method of claim 7, wherein X is a macromolecular carrier group.

34. The method of claim 33, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

35. The method of claim 7, wherein Z is a macromolecular carrier group.

36. The method of claim 35, wherein th e macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

37. The method of claim 7, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

38. The method of claim 37, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

39. The method of claim 7, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

40. The method of claim 7, wherein X is an acetyl group, and Z is an amido group.

41. The method of claim 33, wherein the macromolecular carrier group X is a peptide group.

42. The method of claim 35, wherein the macromolecular carrier group Z is a peptide group.

43. The method of claim 42, wherein X is a peptide macromolecular carrier group and Z is a peptide macromolecular carrier group.

44. The method of claim 7, wherein X is an amino group.

45. The method of claim 7, wherein Z is a carboxyl group.

46. The method of claim 7, wherein X is a 9-fluorenylmethoxy-carbonyl group.

47. The method of claim 8, further comprising administering to the individual a pharmaceutically acceptable carrier.

48. The method of claim 8, wherein X is a hydrophobic group.

49. The method of claim 48, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

50. The method of claim 8, wherein Z is a hydrophobic group.

51. The method of claim 50, wherein the hydrophobic group Z is t-butyloxycarbonyl.

52. The method of claim 8, wherein X is a macromolecular carrier group.

53. The method of claim 52, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

54. The method of claim 8, wherein Z is a macromolecular carrier group.

55. The method of claim 54, wherein the macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

56. The method of claim 8, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

57. The method of claim 56, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

58. The method of claim 8, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

59. The method of claim 8, wherein X is an acetyl group, and Z is an amido group.

60. The method of claim 52, wherein the macromolecular carrier group X is a peptide group.

61. The method of claim 54, wherein the macromolecular carrier group Z is a peptide group.

62. The method of claim 61, wherein X is a peptide macromolecular carrier group and Z is a peptide macromolecular carrier group.

63. The method of claim 8, wherein X is an amino group.

64. The method of claim 8, wherein Z is a carboxyl group.

65. The method of claim 8, wherein X is a 9-fluorenylmethoxy-carbonyl group.

66. The method of claim 9, further comprising administering to the patient a pharmaceutically acceptable carrier.

67. The method of claim 9, wherein X is a hydrophobic group.

68. The method of claim 67, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

69. The method of claim 9, wherein Z is a hydrophobic group.

70. The method of claim 69, wherein the hydrophobic group Z is t-butyloxycarbonyl.

71. The method of claim 9, wherein X is a macromolecular carrier group.

72. The method of claim 71, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

73. The method of claim 9, wherein Z is a macromolecular carrier group.

74. The method of claim 73, wherein the macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

75. The method of claim 9, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

76. The method of claim 75, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

77. The method of claim 9, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

78. The method of claim 9, wherein X is an acetyl group, and Z is an amido group.

79. The method of claim 71, wherein the macromolecular carrier group X is a peptide group.

80. The method of claim 73, wherein the macromolecular carrier group Z is a peptide group.

81. The method of claim 80, wherein X is a peptide macromolecular carrier group and Z is a peptide macromolecular carrier group.

82. The method of claim 9, wherein X is an amino group.

83. The method of claim 9, wherein Z is a carboxyl group.

84. The method of claim 9, wherein X is a 9-fluorenylmethoxy-carbonyl group.

85. The method of claim 1, wherein X is a hydrophobic group.

86. The method of claim 85, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

87. The method of claim 1, wherein Z is a hydrophobic group.

88. The method of claim 87, wherein the hydrophobic group Z is t-butyloxycarbonyl.

89. The method of claim 1, wherein X is a macromolecular carrier group.

90. The method of claim 89, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety, or a peptide group.

91. The method of claim 1, wherein Z is a macromolecular carrier group.

92. The method of claim 91, wherein the macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety, or a peptide group.

93. The method of claim 1, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

94. The method of claim 93, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

95. The method of claim 1, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

96. The method of claim 1, wherein X is a peptide macromolecular carrier group.

97. The method of claim 1, wherein Z is a peptide macromolecular carrier group.

98. The method of claim 1, wherein X is a peptide macromolecular carrier group X , and further wherein Z is a peptide macromolecular carrier group.

99. The method of claim 7, further comprising administering to the individual a pharmaceutically acceptable carrier.

100. A method for inhibiting syncytia formation between HIV-1 infected cells and cells uninfected by HIV-1, comprising contacting the infected cells for an effective period of time with an effective amount of a peptide having the formula:

in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

101. The method of claim 100, wherein X is a hydrophobic group.

102. The method of claim 101, wherein the hydrophobic group X is carbobenzoxyl, dansyl, or t-butyloxycarbonyl.

103. The method of claim 100, wherein Z is a hydrophobic group.

104. The method of claim 103, wherein the hydrophobic group Z is t-butyloxycarbonyl.

105. The method of claim 100, wherein X is a macromolecular carrier group.

106. The method of claim 106, wherein the macromolecular carrier group X is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

107. The method of claim 100, wherein Z is a macromolecular carrier group.

108. The method of claim 108, wherein the macromolecular carrier group Z is a lipid-fatty acid conjugate, a polyethylene glycol, or a carbohydrate moiety.

109. The method of claim 100, wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.

110. The method of claim 110, wherein the non-peptide bond is an imino, ester, hydrazine, semicarbazide, or azo bond.

111. The method of claim 100, wherein at least one amino acid residue of the peptide is in a D-isomer configuration.

112. The method of claim 100, wherein X is an acetyl group, and Z is an amido group.

113. The method of claim 100, wherein X is a peptide macromolecular carrier group.

114. The method of claim 100, wherein Z is a peptide macromolecular carrier group.

115. The method of claim 100, wherein X is a peptide macromolecular carrier group and Z is a peptide macromolecular carrier group.

116. The method of claim 100, wherein X is an amino group.

117. The method of claim 100, wherein Z is a carboxyl group.

118. The method of claim 100, wherein X is a 9-fluorenylmethoxy-carbonyl group.
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