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

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Details

C530S317000, C530S334000

Reexamination Certificate

active

11224819

ABSTRACT:
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 compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is 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, has 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: WO96/23813 (1996-08-01), None
patent: WO98/02176 (1998-01-01), None
Roller, et al., Peptides 1998, Proceedings of the European Peptide Symposium, 25th , Budapest, Aug. 30-Sep. 4, 1998, 706-707.
Jain, Science 271 :1079-1080, 1996, p. 1080.
Dermer, Biocechonology, 1994, 12 : 320.
Gura, Science, 1997, vol. 278, 1041.
Landon et al.,J. Cell. Biochem., 90, 509-517 (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).
Lung et al.,Biopolymers, 71, 132-140 (2003).
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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