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US 2004/0171534 A1Published application
GRF analogs with increased biological potency
AssigneeTheratechnologies Inc.
InventorsDenis Gravel, Abdelkrim Habi, Paul Brazeau
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Abstract
The present invention relates to chimeric fatty body-GRF analogs with increased biological potency, their application as anabolic agents and in the diagnosis and treatment of growth hormone deficiencies. The chimeric fatty body-GRF analogs include an hydrophobic moiety (tail), and can be prepared, either by anchoring at least one hydrophobic tail to the GRF, in the chemical synthesis of GRF. The GRF analogs of the present invention are biodegradable, non-immunogenic and exhibit an improved anabolic potency with a reduced dosage and prolonged activity.
Claims11
An hydrophobic GRF analog of formula A:
- X-GRF-peptide (A)
- wherein;
- the GRF peptide is a peptide of formula B;
- A1-A2-Asp-Ala-Ile-Phe-Thr-A8-Ser-Tyr-Arg-Lys-A13-Leu-A15-Gln-Leu-A18-Ala-Arg-Lys-Leu-Leu-A24-A25-Ile-A27-A28-Arg-A30-R0 (B)
- wherein,
- A1 is Tyr or His;
- A2 is Val or Ala;
- A8 is Asn or Ser;
- A13 is Val or Ile;
- A15 is Ala or Gly;
- A18 is Ser or Tyr;
- A24 is Gln or His;
- A25 is Asp or Glu;
- A27 is Met, Ile or Nle;
- A28 is Ser or Asn;
- A30 is a bond or any amino acid sequence of 1 up to 15 residues;
- R0 is NH2 or NH—(CH2)n—CONH2, with n=1 to 12 and;
- X is a hydrophobic tail anchored via an amide bond to the N-terminus of the peptide and said hydrophobic tail defining a backbone of 5 to 7 atoms;
- wherein said backbone can be substituted by C1-6 alkyl, C3-6 cycloalkyl, or C6-12 aryl;
- and comprises at least one rigidifying moiety connected to at least two atoms of the backbone;
- said moiety selected from the group consisting of double bond, triple bond, saturated or unsaturated C3-9 cycloalkyl, and C6-12 aryl.
18 more elements
Dependencies are inferred from the claim text.