Modified peptides as therapeutic agents
First Claim
Patent Images
1. A composition of matter of the formula
(X1)a—
- F1—
(X2)band multimers thereof, wherein;
F1 is an Fc domain;
X1 and X2 are each independently selected from -(L1)c-P1, -(L1)c-P1-(L2)d-P2, -(L1)c-P1-(L2)d-P2-(L3)e-P3, and -(L1)c-P1-(L2)d-P2-(L3)e-P3-(L4)f-P4 P1, P2, P3, and P4 are each independently randomized TPO-mimetic peptide sequences;
L1, L2, L3, and L4 are each independently linkers; and
a, b, c, d, e, and f are each independently 0 or 1, provided that at least one of a and b is 1 and wherein “
peptide”
refers to molecules 2 to 40 amino acid and wherein neither X1 nor X2 is a native protein.
0 Assignments
0 Petitions
Accused Products
Abstract
The present invention concerns fusion of Fc domains with biologically active peptides and a process for preparing pharmaceutical agents using biologically active peptides. In this invention, pharmacologically active compounds are prepared by a process comprising:
- a) selecting at least one peptide that modulates the activity of a protein of interest; and
- b) preparing a pharmacologic agent comprising an Fc domain covalently linked to at least one amino acid of the selected peptide.
Linkage to the vehicle increases the half-life of the peptide, which otherwise would be quickly degraded in vivo. The preferred vehicle is an Fc domain. The peptide is preferably selected by phage display, E. coli display, ribosome display, RNA-peptide screening, or chemical-peptide screening.
-
Citations
10 Claims
-
1. A composition of matter of the formula
(X1)a—- F1—
(X2)band multimers thereof, wherein; F1 is an Fc domain; X1 and X2 are each independently selected from -(L1)c-P1, -(L1)c-P1-(L2)d-P2, -(L1)c-P1-(L2)d-P2-(L3)e-P3, and -(L1)c-P1-(L2)d-P2-(L3)e-P3-(L4)f-P4 P1, P2, P3, and P4 are each independently randomized TPO-mimetic peptide sequences; L1, L2, L3, and L4 are each independently linkers; and a, b, c, d, e, and f are each independently 0 or 1, provided that at least one of a and b is 1 and wherein “
peptide”
refers to molecules 2 to 40 amino acid and wherein neither X1 nor X2 is a native protein.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
or
F1—
X2.
- F1—
-
3. The composition of matter of claim 1 of the formula
F1-(L1)c-P1. -
4. The composition of matter of claim 1 of the formula
F1-(L1)c-P1-(L2)d-P2. -
5. The composition of matter of claim 1 wherein F1 is an IgG Fc domain.
-
6. The composition of matter of claim 1 wherein F1 is an IgG1 Fc domain.
-
7. The composition of matter of claim 1 wherein F1 comprises the sequence of SEQ ID NO:
- 2.
-
8. The composition of matter of claim 1 wherein P1 is a TPO-mimetic peptide sequence selected from Table 6.
-
9. The composition of matter of claim 8 wherein F1 comprises the sequence of SEQ ID NO:
- 2.
-
10. The composition of matter of claim 1 having a sequence selected from SEQ ID NOS:
- 6 and 12.
Specification