Agonist peptide dimers

Details Agonist peptide dimers Agonist peptide dimers

A - Human Necessities

61

K

A61K 38/16 (2006.01) A61K 38/18 (2006.01) A61K 38/20 (2006.01) A61K 38/28 (2006.01)

Patent

CA 2628032

The present invention is directed to the dimerization of agonists and antagonists of cell surface receptors and particularly to peptide dimers which behave as cell surface receptor agonists in their dimeric form. Such receptors belong to the dimerization- mediated activation class often observed among receptors for growth and differentiation factors. The agonists of this class of receptors is understood to effect dimerization of the receptor and thus signal initiation. The present invention exemplifies dimers of erythropoietin (EPO) agonists and antagonists comprising a core amino acid sequence of X3X4X5GPX6TWX7X8 (SEQ ID NO: 1) wherein each amino acid is indicated by standard one letter abbreviation; X3 can be C, A, .alpha.-amino-.gamma.-bromobutyric acid or Hoc; X4 can be R, H, L or W; X5 can be M, F, or I; X6 is independently selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids; X7 can be D, E, I, L or V; and X8 can be C, A, .alpha.-amino-.gamma.--bromobutyric acid or Hoc, provided that either X3 or X8 is C or Hoc.

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