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EP0255206A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Peptides that inhibit von Willebrand factor binding

Assignee: Scripps Research Institute
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Filing: 1987-05-22
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Granted: —
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Expires: 2007-05-22
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Abstract

Abstract Peptides which inhibit the binding of von Willebrand factor to platelets, heparin and collagen. The method of preventing thrombosis, by administering one or more of these peptides, is also disclosed.

Inventors

  • 👤 Theodore S. Zimmerman
  • 👤 Yoshihiro Fujimura
  • 👤 Richard A. Houghten
  • 👤 Zaverio M. Ruggeri

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 18:19
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/745; C07K14/755; A; A61; A61P; A61P7/00; A61P7/02; A61K; A61K38/00

Claims Analysis

Total Claims: 38
Claim 1
Independent Claim 59 words
A 52/48 kDa polypeptide fragment which inhibits binding of von Willebrand factor to platelets, heparin and collagen and whose amino acid sequence is that of a fragment of von Willebrand factor as follows: a fragment whose amino-terminal sequence begins with amino-terminal amino acid residue 449 Val and whose carboxy-terminal residue extends no further than amino acid residue 729 Arg.
Claim 2
Dependent Claim 59 words
A 52/48 kDa polypeptide fragment which inhibits binding of von Willebrand factor to platelets, heparin and collagen and whose amino acid sequence is that of a fragment of von Willebrand factor as follows: a fragment whose amino-terminal sequence begins with amino-terminal amino acid residue 449 Val and whose carboxy-terminal residue extends no further than amino acid residue 729 Arg.
Claim 3
Dependent Claim 49 words
A peptide which inhibits binding of von Willebrand factor to platelets selected from the group of peptides consisting of: LCDLAPEAPPPTLPP; PEAPPPTLPPDMAQV; VKYAGSQVASTSEVL; SDPEHCQICHCDVVN; CDVVNLTCEACQEPG; CQEPGGLVVPPSDAP; PSDAPVSPSSLYVED; RIASQVKYAGSQVAS; PSELRRIASQVKYAG; DMMERLRISQKWVRV; EFEVLKAFVVDMMER; KAFVVDMMERLRISQ; HDGSHAYIGLKDRKR; QIFSKIDRPEASRIA; LYVEDISEPPLHDFY; VSPSSLYVEDISEPP; AYIGLKDRKRPSELR; KDRKRPSELRRIASQ; ASRIALLLMASQEPQ; RMSRNFVRYVQGLKK; VTLNPSDPEHCQICH; CQICHCDVVNLTCEA; IPVGIGPHANLKQIR; GPHANLKQIRLIEKQ; SVDELEQQRDEIVSY; EIVSYLCDLAPEAPP; PTLPPDMAQVTVGPG; TVGPGLLGVSTLGPK and LKQIRLIEKQAPENK.
Claim 4
Dependent Claim 49 words
A peptide which inhibits binding of von Willebrand factor to platelets selected from the group of peptides consisting of: LCDLAPEAPPPTLPP; PEAPPPTLPPDMAQV; VKYAGSQVASTSEVL; SDPEHCQICHCDVVN; CDVVNLTCEACQEPG; CQEPGGLVVPPSDAP; PSDAPVSPSSLYVED; RIASQVKYAGSQVAS; PSELRRIASQVKYAG; DMMERLRISQKWVRV; EFEVLKAFVVDMMER; KAFVVDMMERLRISQ; HDGSHAYIGLKDRKR; QIFSKIDRPEASRIA; LYVEDISEPPLHDFY; VSPSSLYVEDISEPP; AYIGLKDRKRPSELR; KDRKRPSELRRIASQ; ASRIALLLMASQEPQ; RMSRNFVRYVQGLKK; VTLNPSDPEHCQICH; CQICHCDVVNLTCEA; IPVGIGPHANLKQIR; GPHANLKQIRLIEKQ; SVDELEQQRDEIVSY; EIVSYLCDLAPEAPP; PTLPPDMAQVTVGPG; TVGPGLLGVSTLGPK and LKQIRLIEKQAPENK.
Claim 5
Dependent Claim 13 words
A peptide according to claim 2 wherein said peptide has the sequence LCDLAPEAPPPTLPP.
Claim 6
Dependent Claim 13 words
A peptide according to claim 2, wherein said peptide has the sequence PEAPPPTLPPDMAQV.
Claim 7
Dependent Claim 13 words
A peptide according to claim 2, wherein said peptide has the sequence LYVEDISEPPLHDFY.
Claim 8
Dependent Claim 19 words
A peptide of claim 2 which comprises within the peptide any sequential subset of at least two amino acids.
Claim 9
Dependent Claim 31 words
A peptide which inhibits binding of von Willebrand factor to heparin selected from the group of peptides consisting of: KDRKRPSELRRIASQ; LIEKQAPENKAFVLS; SQEPQRMSRNFURYV; KYTLFQIFSKIDRPE; DMMERLRISQKWVRV; LYVEDISEPPLHDFY; ISEPPLHDFYCSRLL; SQEPQRMSRNFVRYV; IPVGIGPHANLKQIR; GPHANLKQIRLIEKQ; and TVGPGLLGVSTLGPK.
Claim 10
Dependent Claim 31 words
A peptide which inhibits binding of von Willebrand factor to heparin selected from the group of peptides consisting of: KDRKRPSELRRIASQ; LIEKQAPENKAFVLS; SQEPQRMSRNFURYV; KYTLFQIFSKIDRPE; DMMERLRISQKWVRV; LYVEDISEPPLHDFY; ISEPPLHDFYCSRLL; SQEPQRMSRNFVRYV; IPVGIGPHANLKQIR; GPHANLKQIRLIEKQ; and TVGPGLLGVSTLGPK.
Claim 11
Dependent Claim 13 words
A peptide according to claim 7, wherein said peptide has the sequence KDRKRPSELRRIASQ.
Claim 12
Dependent Claim 19 words
A peptide of claim 7 which comprises within the peptide any sequential subset of at least two amino acids.
Claim 13
Dependent Claim 20 words
A peptide as set out in any one of claims 2-6, further comprising repeating sequences of any of the peptides.
Claim 14
Dependent Claim 20 words
A peptide as set out in any one of claims 7-9, further comprising repeating sequences of any of the peptides.
Claim 15
Dependent Claim 20 words
A peptide as set out in any one of claims 2-6, further comprising any combination of any of the peptides.
Claim 16
Dependent Claim 20 words
A peptide as set out in any one of claims 7-9, further comprising any combination of any of the peptides.
Claim 17
Dependent Claim 28 words
A peptide as set out in any one of claims 2-6, further comprising at least one amino acid R extending from the amino or carboxy-terminus of said peptide.
Claim 18
Dependent Claim 28 words
A peptide as set out in any one of claims 7-9, further comprising at least one amino acid R extending from the amino or carboxy-terminus of said peptide.
Claim 19
Dependent Claim 28 words
A peptide as set out in any one of claims 2-6, further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 20
Dependent Claim 28 words
A peptide as set out in any one of claims 7-9, further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 21
Dependent Claim 32 words
A peptide as set out in any one of claims 2-6, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 22
Dependent Claim 32 words
A peptide as set out in any one of claims 7-9, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 23
Dependent Claim 25 words
A peptide as set out in claim 10, further comprising at least one amino acid R extending from the amino or carboxy-terminus of said peptide.
Claim 24
Dependent Claim 25 words
A peptide as set out in claim 11, further comprising at least one amino acid R extending from the amino or carboxy-terminus of said peptide.
Claim 25
Dependent Claim 25 words
A peptide as set out in claim 12, further comprising at least one amino acid R extending from the amino or carboxy-terminus of said peptide.
Claim 26
Dependent Claim 19 words
A peptide as set out in claim 13, further comprising at least one amino or carboxy-terminus of said peptide.
Claim 27
Dependent Claim 25 words
A peptide as set out in claim 10, further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 28
Dependent Claim 25 words
A peptide as set out in claim 11, further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 29
Dependent Claim 25 words
A peptide as set out in claim 12, further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 30
Dependent Claim 25 words
A peptide as set out in claim 13 further comprising at least one amino acid K extending from the amino or carboxy-terminus of said peptide.
Claim 31
Dependent Claim 29 words
A peptide as set out in claim 10, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 32
Dependent Claim 29 words
A peptide as set out in claim 11, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 33
Dependent Claim 29 words
A peptide as set out in claim 12, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 34
Dependent Claim 29 words
A peptide as set out in claim 13, further comprising at least one combination of amino acids R and K extending from the amino or carboxy-terminus of said peptide.
Claim 35
Dependent Claim 39 words
A therapeutic composition comprising an amount of a 52/48 KDa polypeptide fragment according to claim 1 effective to inhibit binding of von Willebrand factor to platelets, heparin and collagen in a patient, in association with a pharmaceutically acceptable carrier.
Claim 36
Dependent Claim 67 words
A therapeutic composition comprising an amount of one or more peptides according to anyone of claims 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, or 31, effective to inhibit binding of von Willebrand factor to platelets in a patient, in association with a pharmaceutically acceptable carrier.
Claim 37
Dependent Claim 24 words
A method of inhibiting thrombosis in a patient which comprises administering to such patient an effective amount of a polypeptide according to claim 1.
Claim 38
Independent Claim 57 words
A method of inhibiting thrombosis in a patient which comprises administering to such patient an effective amount of a peptide according to any one of claims 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30 or 31.

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