US2002165159A1PendingUtilityA1
FSH-releasing peptides
Est. expiryJun 4, 2017(expired)· nominal 20-yr term from priority
C07K 14/575A61K 38/00C07K 7/23
51
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Claims
Abstract
Lamprey LHRH-III is a potent FSH-releasing factor, and may be used to enhance fertility. Antagonists to lamprey LHRH-III may be used to inhibit fertility.
Claims
exact text as granted — not AI-modifiedWhat is claimed:
1 . A method of altering the level of secretion of FSH in a vertebrate animal, comprising administering to the animal an effective amount of a peptide selected from the group consisting of an l-LHRH-III agonist peptide; an l-LHRH-III superagonist peptide; an l-LHRH-III antagonist peptide; a peptide selected from the group consisting of SEQ. ID NO. 6 through SEQ. ID NO. 41; and l-LHRH-III (SEQ. ID NO. 1); wherein the amount of the peptide administered causes a selective change in the serum FSH level of the animal, but does not cause a proportional change in the serum LH level of the animal.
2 . A method as recited in claim 1 , wherein the level of secretion of FSH in the animal is increased; said method comprising administering to the animal an effective amount of l-LHRH-III (SEQ. ID No. 1).
3 . A method as recited in claim 2 , wherein the animal is a mammal.
4 . A method as recited in claim 3 , wherein the animal is a human.
5 . A method as recited in claim 4 , wherein the human is male.
6 . A method as recited in claim 4 , wherein the human is female.
7 . A method of increasing the fertility of a vertebrate animal, comprising increasing the level of FSH secretion in the animal by the method of claim 2 .
8 . A method as recited in claim 7 , wherein the animal is a mammal.
9 . A method as recited in claim 8 , wherein the animal is a human.
10 . A method as recited in claim 9 , wherein the human is male.
11 . A method as recited in claim 9 , wherein the human is female.
12 . A method as recited in claim 1 , wherein the level of secretion of FSH in the animal is increased; said method comprising administering to the animal an effective amount of an l-LHRH-III agonist peptide or l-LHRH-III superagonist peptide; wherein the amount of the peptide administered causes a selective increase in the serum FSH level of the animal, but does not cause a proportional increase in the serum LH level of the animal.
13 . A method as recited in claim 12 , wherein the peptide is selected from the group consisting of decapeptides whose sequences are identical to the sequence of l-LHRH-III (SEQ. ID NO. 1), except that either or both of the following conditions is satisfied:
(a) the sixth amino acid residue is a natural or xenobiotic amino acid residue other than aspartic acid; or (b) the ninth amino acid residue is prolyl ethyl amide (ProNHEt); and the tenth amino acid residue of l-LHRH-III is deleted.
14 . A method as recited in claim 13 , wherein the peptide is selected from the group consisting of SEQ. ID NO. 6 through SEQ. ID NO. 32.
15 . A method as recited in claim 12 , wherein the animal is a mammal.
16 . A method as recited in claim 15 , wherein the animal is a human.
17 . A method as recited in claim 16 , wherein the human is male.
18 . A method as recited in claim 16 , wherein the human is female.
19 . A method of increasing the fertility of a vertebrate animal, comprising increasing the level of FSH secretion in the animal by the method of claim 12 .
20 . A method as recited in claim 19 , wherein the peptide is selected from the group consisting of decapeptides whose sequences are identical to the sequence of l-LHRH-III (SEQ. ID NO. 1), except that either or both of the following conditions is satisfied:
(a) the sixth amino acid residue is a natural or xenobiotic amino acid residue other than aspartic acid; or (b) the ninth amino acid residue is prolyl ethyl amide (ProNHEt); and the tenth amino acid residue of l-LHRH-III is deleted.
21 . A method as recited in claim 20 , wherein the peptide is selected from the group consisting of SEQ. ID NO. 6 through SEQ. ID NO. 32.
22 . A method as recited in claim 19 , wherein the animal is a mammal.
23 . A method as recited in claim 19 , wherein the animal is a human.
24 . A method as recited in claim 23 , wherein the human is male.
25 . A method as recited in claim 23 , wherein the human is female.
26 . A method as recited in claim 1 , wherein the level of secretion of FSH in the animal is decreased; said method comprising administering to the animal an effective amount of an l-LHRH-III antagonist peptide; wherein the amount of the peptide administered causes a selective decrease in the serum FSH level of the animal, but does not cause a proportional decrease in the serum LH level of the animal.
27 . A method as recited in claim 26 , wherein the antagonist is selected from the group consisting of SEQ. ID NO. 33 through SEQ. ID NO. 41.
28 . A method as recited in claim 26 , wherein the animal is a mammal.
29 . A method as recited in claim 28 , wherein the animal is a human.
30 . A method as recited in claim 29 , wherein the human is male.
31 . A method as recited in claim 29 , wherein the human is female.
32 . A method of decreasing the fertility of a vertebrate animal, comprising decreasing the level of FSH secretion in the animal by the method of claim 26 .
33 . A method as recited in claim 32 , wherein the antagonist is selected from the group consisting of SEQ. ID NO. 33 through SEQ. ID NO. 41.
34 . A method as recited in claim 32 , wherein the animal is a mammal.
35 . A method as recited in claim 34 , wherein the animal is a human.
36 . A method as recited in claim 35 , wherein the human is male.
37 . A method as recited in claim 35 , wherein the human is female.
38 . A composition selected from the group consisting of an l-LHRH-III agonist peptide; an l-LHRH-III superagonist peptide; an I-LHRH-III antagonist peptide; a peptide selected from the group consisting of SEQ. ID NO. 6 through SEQ. ID NO. 41; and an effective amount of substantially pure l-LHRH-III (SEQ. ID NO. 1) admixed with a pharmaceutically acceptable carrier; wherein said composition has the property that said composition will, when administered in an effective amount to a vertebrate animal, cause a selective change in the serum FSH level of the animal, but will not cause a proportional change in the serum LH level of the animal.
39 . A composition as recited in claim 38 , wherein said composition comprises an effective amount of substantially pure l-LHRH-III (SEQ. ID NO. 1) admixed with a pharmaceutically acceptable carrier.
40 . A composition as recited in claim 38 , wherein said composition comprises a peptide selected from the group consisting of SEQ. ID NO. 6 through SEQ. ID NO. 32.
41 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 6.
42 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 7.
43 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 8.
44 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 9.
45 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 10.
46 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 11.
47 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 12.
48 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 13.
49 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 14.
50 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 15.
51 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 16.
52 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 17.
53 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 18.
54 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 19.
55 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 20.
56 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 21.
57 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 22.
58 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 23.
59 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 24.\
60 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 25.
61 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 26.
62 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 27.
63 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 28.
64 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 29.
65 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 30.
66 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 31.
67 . A peptide as recited in claim 40 , wherein said peptide is SEQ. ID NO. 32.
68 . A composition as recited in claim 38 , wherein said composition comprises a peptide selected from the group consisting of SEQ. ID NO. 33 through SEQ. ID NO. 41.
69 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 33.
70 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 34.
71 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 35.
72 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 36.
73 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 37.
74 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 38.
75 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 39.
76 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 40.
77 . A peptide as recited in claim 68 , wherein said peptide is SEQ. ID NO. 41.Join the waitlist — get patent alerts
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