Redox-stable, non-phosphorylated cyclic peptide inhibitors...

Details Redox-stable, non-phosphorylated cyclic peptide inhibitors... Redox-stable, non-phosphorylated cyclic peptide inhibitors...

2005-10-04

2005-10-04

Andres, Janet (Department: 1646)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

C530S333000, C514S001000, C514S009100

Reexamination Certificate

active

06951915

ABSTRACT:
A compound of formula:in which L is sulfur, sulfoxide, oxygen or methylene, and a compound of formula:in which (i) aa1is Adi and aa4is Glu or (ii) each of aa1and aa4is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compounds (and their conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, are non-phosphorylated, are redox-stable in vivo, are characterized by an IC50in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, have a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.

REFERENCES:
patent: WO 96/23813 (1996-08-01), None
patent: WO 98/02176 (1998-01-01), None
Landon et.al., J. Cell. Biochem. 90:509-517 (2003).
Lung et.al., Biopolymers 71:132-140 (2003).
Long et al. “Significant Compensatory Role of Position Y-2 Conferring High Affinity to Non-Phosphorylated Inhibitors of GRB2-SH2 Domain”Bioorganic&Medicinal Chemistry Letters, 9 (15), 2267-2272, (Aug. 2, 1999).
Long et al. “Structural Requirements for Tyr in the Consensus Sequence Y-E-N of a Novel Nonphosphorylated inhibitor to the Grb2-SH2 Domain”Biochemical and Biophysical Research Communications, 264 (3), 902-908 (1999).
Lung et al. “Novel Non-Phosphorylated Peptides Binding to the Grb2-SH2 Domain”Proceedings of the American Peptide Symposium(1997).
Oligino et al. “Nonphosphorylated Peptide Ligands for the Grb2 Src Homology 2 Domain”Journal of Biological Chemistry, 272 (46), 29046-29052, (Nov. 14, 1997).

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