JP2014524902A5 - - Google Patents

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Publication number

JP2014524902A5

JP2014524902A5 JP2014515968A JP2014515968A JP2014524902A5 JP 2014524902 A5 JP2014524902 A5 JP 2014524902A5 JP 2014515968 A JP2014515968 A JP 2014515968A JP 2014515968 A JP2014515968 A JP 2014515968A JP 2014524902 A5 JP2014524902 A5 JP 2014524902A5

Authority

JP

Japan

Prior art keywords

seq

antigen

binding fragment

antibody

amino acid

Prior art date

2012-06-13

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

Links

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• 125000003275 alpha amino acid group Chemical group 0.000 claims description 61
• 239000012634 fragment Substances 0.000 claims description 40
• 239000000427 antigen Substances 0.000 claims description 37
• 102000036639 antigens Human genes 0.000 claims description 37
• 108091007433 antigens Proteins 0.000 claims description 37
• 150000001413 amino acids Chemical class 0.000 claims description 33
• 238000000034 method Methods 0.000 claims description 29
• 206010028980 Neoplasm Diseases 0.000 claims description 20
• 210000002889 endothelial cell Anatomy 0.000 claims description 18
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 16
• 239000003053 toxin Substances 0.000 claims description 15
• 231100000765 toxin Toxicity 0.000 claims description 15
• 102100031323 Anthrax toxin receptor 1 Human genes 0.000 claims description 11
• 210000004027 cell Anatomy 0.000 claims description 11
• 239000002246 antineoplastic agent Substances 0.000 claims description 10
• 229940127089 cytotoxic agent Drugs 0.000 claims description 10
• 108010047041 Complementarity Determining Regions Proteins 0.000 claims description 8
• 239000012636 effector Substances 0.000 claims description 8
• 239000003550 marker Substances 0.000 claims description 8
• 241000193738 Bacillus anthracis Species 0.000 claims description 6
• 101710194807 Protective antigen Proteins 0.000 claims description 6
• 239000004037 angiogenesis inhibitor Substances 0.000 claims description 6
• 230000015572 biosynthetic process Effects 0.000 claims description 6
• 108010044540 auristatin Proteins 0.000 claims description 5
• MFRNYXJJRJQHNW-DEMKXPNLSA-N (2s)-2-[[(2r,3r)-3-methoxy-3-[(2s)-1-[(3r,4s,5s)-3-methoxy-5-methyl-4-[methyl-[(2s)-3-methyl-2-[[(2s)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 MFRNYXJJRJQHNW-DEMKXPNLSA-N 0.000 claims description 4
• 208000034038 Pathologic Neovascularization Diseases 0.000 claims description 4
• IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims description 4
• 108010093470 monomethyl auristatin E Proteins 0.000 claims description 4
• 108010059074 monomethylauristatin F Proteins 0.000 claims description 4
• 238000000338 in vitro Methods 0.000 claims description 3
• 206010006187 Breast cancer Diseases 0.000 claims description 2
• 208000026310 Breast neoplasm Diseases 0.000 claims description 2
• 206010009944 Colon cancer Diseases 0.000 claims description 2
• 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
• 102000004190 Enzymes Human genes 0.000 claims description 2
• 108090000790 Enzymes Proteins 0.000 claims description 2
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
• 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
• 239000012472 biological sample Substances 0.000 claims description 2
• 238000001514 detection method Methods 0.000 claims description 2
• 239000003937 drug carrier Substances 0.000 claims description 2
• 229910001385 heavy metal Inorganic materials 0.000 claims description 2
• 201000005202 lung cancer Diseases 0.000 claims description 2
• 208000020816 lung neoplasm Diseases 0.000 claims description 2
• 230000002285 radioactive effect Effects 0.000 claims description 2
• 201000000849 skin cancer Diseases 0.000 claims description 2
• 101000796095 Homo sapiens Anthrax toxin receptor 1 Proteins 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 150000007523 nucleic acids Chemical class 0.000 claims 3
• 102000039446 nucleic acids Human genes 0.000 claims 3
• 108020004707 nucleic acids Proteins 0.000 claims 3
• 238000004519 manufacturing process Methods 0.000 claims 2
• 230000001772 anti-angiogenic effect Effects 0.000 claims 1
• 229960000397 bevacizumab Drugs 0.000 claims 1
• 230000003472 neutralizing effect Effects 0.000 claims 1
• 125000000539 amino acid group Chemical group 0.000 description 12
• 101710125943 Anthrax toxin receptor 1 Proteins 0.000 description 6
• 239000003795 chemical substances by application Substances 0.000 description 3
• 201000009030 Carcinoma Diseases 0.000 description 2
• GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 2
• 239000002771 cell marker Substances 0.000 description 2
• 229960002949 fluorouracil Drugs 0.000 description 2
• 229960004768 irinotecan Drugs 0.000 description 2
• UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 description 2
• 102000005600 Cathepsins Human genes 0.000 description 1
• 108010084457 Cathepsins Proteins 0.000 description 1
• 206010053614 Type III immune complex mediated reaction Diseases 0.000 description 1
• 230000016178 immune complex formation Effects 0.000 description 1
• 238000001727 in vivo Methods 0.000 description 1