Leptin antagonists

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues

Reexamination Certificate

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Details

C436S086000, C514S012200, C514S773000, C435S069100

Reexamination Certificate

active

10996607

ABSTRACT:
The invention relates to synthetic leptin antagonists in which at least two amino acid residues of the sequence LDFI/S of the hydrophobic binding site at positions39-42of a leptin polypeptide sequence are substituted with different amino acid residues such that the site becomes less hydrophobic, and fragments of said leptin antagonists.

REFERENCES:
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patent: 6399745 (2002-06-01), Ertl et al.
patent: 2004/0048773 (2004-03-01), Cawthorne et al.
patent: 2004/0072219 (2004-04-01), Carr et al.
patent: 2292382 (1996-02-01), None
patent: WO 02/062833 (2002-08-01), None
Peelman et al., “Mapping of the leptin binding sites and design of a leptin antagonist” (2004) J. Biol Chem., vol. 279; pp. 4138-4146.
Raver et al., “Comparison of R128Q mutations in human, ovine, and chicken leptois” (2002) General and Comparative Endocrinology, vol. 126, pp. 52-58.
Verploegen et al., “A human leptin mutant induces weight gain in normal mice” (1997) FEBS Letters, vol. 405, pp. 237-240.
Zabeau et al., “Functional analysis of leptin receptor activation using a Janus kinase/signal transducer and activator of transcription complementation assay” (2004) Molecular Endocrinology, vol. 18 No. 1, pp. 150-161.

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