Peptide inhibitors of bace1
AssigneesGenentech, Inc., F. Hoffman-La Roche AG
InventorsRobert A. Lazarus, Yingnan Zhang, Weiru Wang
Life of this patent
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Abstract
The invention provides peptide inhibitors of BACE1 that bind to the active site in a noncanonical fashion, and methods of use thereof.
Claims43
An isolated polypeptide that binds specifically to BACE1, wherein the polypeptide comprises the amino acid sequence X1-S-X2-Y-C-R-L-X3-X4-X5-X6-C-(X7)n (SEQ ID NO:
- 6), wherein X1 is glutamic acid or aspartic acid;
- wherein X2 is methionine, leucine, isoleucine or valine;
- wherein X3 is leucine or methionine;
- wherein X4 is glycine, serine or alanine;
- wherein X5 is leucine, isoleucine or valine;
- wherein X6 is glycine or alanine;
- wherein X7 is glycine, aspartic acid or glutamic acid, and wherein n is 0 or 1.
-8. (canceled)
-13. (canceled)
An isolated polypeptide consisting essentially of an amino acid sequence selected from the group consisting of KEESIYCRLMGLGCG (SEQ ID NO:
- 14), NELSPYCRLMGLGCD (SEQ ID NO:
- 15), NEESMYCRLLGIGCG (SEQ ID NO:
- 16) and PEESLYCRLLALGCG (SEQ ID NO:
- 17).
-18. (canceled)
An isolated polypeptide that binds specifically to BACE1, wherein the polypeptide comprises the amino acid sequence SMYCRLLGIGCG (SEQ ID NO:
- 18) (BACE031) or ESMYCRLLGIGCG (SEQ ID NO:
- 19) (BACE030).
(canceled)
(canceled)
An isolated polypeptide that binds specifically to BACE1, wherein the polypeptide comprises a sequence having cysteines at positions −1 and −8 relative to the C terminus, an arginine or arginine analogue at position −7 relative to the C-terminus, and a leucine at position −6 relative to the C-terminus.
(canceled)
-33. (canceled)
(canceled)
An isolated polypeptide that binds specifically to BACE1 and comprises a C-terminal, N-terminal, or internal amino acid sequence comprising the amino acid sequence of a peptide selected from the amino acid sequences set forth in Table 2 and FIG. 2.
-68. (canceled)
Dependencies are inferred from the claim text.