Compositions and methods for promoting lipid mobilization in humans
AssigneeBLM Group
InventorsBernice Schacter, Lee P. Schacter
Life of this patent
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Abstract
The invention provides methods of using polypeptide compounds based on the structures of insect peptides of the adipokinetic hormone family to mobilize lipids in humans. The compositions and methods described in the application are useful for modulating human body weight, such as inducing weight loss. The invention also includes screening methods for identifying other compounds effective for modulating lipid mobilization in humans.
Claims57
1-29. (canceled)
A method of promoting lipid mobilization in a human, the method comprising administering to the human, in an amount effective to mobilize lipids in the human, a compound having the chemical structure
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
- or a physiologically acceptable salt thereof
- wherein:
- Xaa1 is a glutamate residue, a pyroglutamate residue or a glutamine residue;
- Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
- Xaa3 is one of an asparagine residue and a threonine residue;
- Xaa4 is one of a phenylalanine residue and a tyrosine residue;
- Xaa5 is one of a threonine residue and a serine residue;
- Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
- Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
- Xaa8 is a tryptophan residue;
- X is from 0 to 10 amino acid residues;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
31-46. (canceled)
A method of promoting lipid mobilization in a human, the method comprising administering to the human, in an amount effective to mobilize lipids in the human, a compound having the chemical structure
- Xaa1-Xaa22-Xaa23-Xaa24-Xaa25-Xaa26-Xaa27-Xaa28-X-Z,
- or a physiologically acceptable salt thereof
- wherein:
- Xaa1 is a glutamate residue, a pyroglutamate residue or glutamine residue;
- Xaa22 is an amino acid residue having a non-polar side chain;
- Xaa23 is an amino acid residue having a non-ionic polar side chain;
- Xaa24 is an amino acid residue having an aromatic side chain;
- Xaa25 is an amino acid residue having a non-ionic polar side chain;
- Xaa26 is any amino acid residue;
- Xaa27 is any amino acid residue;
- Xaa28 is an amino acid residue having an aromatic side chain;
- X is from 0 to 10 amino acid residues;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
A method of promoting lipid mobilization in a human, the method comprising administering to the human in an amount effective to mobilize lipids in the human, a compound having the chemical structure
- Xaa1-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Z.
- or a physiologically acceptable salt thereof
- wherein:
- Xaa1 is a glutamate residue, a pyroglutamate residue or a glutamine residue;
- Xaa3 is one of an asparagine residue and a threonine residue;
- Xaa4 is one of a phenylalanine residue and a tyrosine residue;
- Xaa5 is one of a threonine residue and a serine residue;
- Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
- Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
- Xaa8 is a tryptophan residue;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
A method of promoting lipid mobilization in a human, the method comprising administering to the human in an amount effective to mobilize lipids in the human, a compound having the chemical structure
- Xaa1-Xaa3-Xaa4-Xaa5-Xaa6-Lys-Z,
- or a physiologically acceptable salt thereof
- wherein:
- Xaa1 is a glutamate residue, a pyroglutamate residue or a glutamine residue;
- Xaa3 is one of an asparagine residue and a threonine residue;
- Xaa4 is one of a phenylalanine residue and a tyrosine residue;
- Xaa5 is one of a threonine residue and a serine residue;
- Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
A method of treating a human afflicted with one or more of obesity, overweight, type II diabetes, cholelithiasis, hypertension, coronary heart disease, arthritis, cancer, renal failure, liver disease, chronic pain, sleep apnea, stroke, urinary incontinence, atherosclerosis, coronary artery disease, high blood pressure, cardiac insufficiency or stroke comprising administering to the human, an effective amount of a compound having the chemical structure
- Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-X-Z,
- or a physiologically acceptable salt thereof
- wherein:
- Xaa1 is a glutamate residue, a pyroglutamate residue or glutamine residue;
- Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
- Xaa3 is one of an asparagine residue and a threonine residue;
- Xaa4 is one of a phenylalanine residue and a tyrosine residue;
- Xaa5 is one of a threonine residue and a serine residue;
- Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
- Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
- Xaa8 is a tryptophan residue;
- X is from 0 to 10 amino acid residues;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
A method of promoting lipid mobilization in a human, the method comprising administering to the human, in an amount effective to mobilize lipids in the human, a polypeptide of between 8 and 18 amino acids comprising the chemical structure
- Xaa2-Xaa3-Xaa4-Xaa8-Xaa6-Xaa7-Xaa8-X-Z,
- or a physiologically acceptable salt thereof
- wherein:
- Xaa2 is one of a leucine residue, an isoleucine residue, a valine residue, a phenylalanine residue, and a tyrosine residue;
- Xaa3 is one of an asparagine residue and a threonine residue;
- Xaa4 is one of a phenylalanine residue and a tyrosine residue;
- Xaa5 is one of a threonine residue and a serine residue;
- Xaa6 is one of a proline residue, a serine residue, a threonine residue, and an alanine residue;
- Xaa7 is one of glycine residue, an asparagine residue, a serine residue, an aspartate residue, a valine residue, and a tryptophan residue;
- Xaa8 is a tryptophan residue;
- X is from 0 to 10 amino acid residues;
- and
- Z is one of a hydrogen radical and a carboxyl terminus-blocking moiety.
Dependencies are inferred from the claim text.