Rational humanization of the powerful antithrombotic anti-GPIbα antibody: 6B4

Thrombosis and Haemostasis

Volumn 96, Issue 5, 2006, Pages 671-684

  Fontayne, Alexandre ^a   Vanhoorelbeke, Karen ^a   Pareyn, Inge ^a   Van Rompaey, Isabel ^b   Meiring, Muriel ^c   Lamprecht, Seb ^c   Roodt, Jan ^c   Desmet, Johan ^d   Deckmyn, Hans ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

^b Thromb X NV   (Belgium)

^c UNIVERSITY OF THE FREE STATE   (South Africa)

^d Algonomics   (Belgium)

Author keywords

Antithrombotic; Computer modeling; Glycoprotein lb; Humanization; Platelet

Indexed keywords

ANTICOAGULANT AGENT; GLYCOPROTEIN IB ALPHA; IMMUNOGLOBULIN F(AB) FRAGMENT; MONOCLONAL ANTIBODY; MONOCLONAL ANTIBODY 6B4; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBODY AFFINITY; ANTIGEN ANTIBODY COMPLEX; ANTIGEN BINDING; ARTICLE; COMPUTER AIDED DESIGN; COMPUTER MODEL; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG MECHANISM; DRUG PURIFICATION; DRUG STRUCTURE; ENZYME LINKED IMMUNOSORBENT ASSAY; GENE CONSTRUCT; GENE EXPRESSION; GENE SEQUENCE; GENE STRUCTURE; GENETIC CODE; HEAVY CHAIN; HUMAN; HUMAN CELL; IN VITRO STUDY; LIGHT CHAIN; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DETERMINATION; PROTEIN DOMAIN; PROTEIN STRUCTURE; SEQUENCE HOMOLOGY; SURFACE PLASMON RESONANCE;

ANIMALS; ANTIBODIES, MONOCLONAL; CLONING, MOLECULAR; COMPUTER SIMULATION; DRUG DESIGN; FIBRINOLYTIC AGENTS; HUMANS; IMMUNOGLOBULIN FAB FRAGMENTS; MICE; MODELS, MOLECULAR; PAPIO; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX; PROTEIN CONFORMATION; PROTEIN ENGINEERING;

EID: 33751251972     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1160/TH06-06-0297     Document Type: Article

References (36)

1. Kohler G, Milstein C. Continuous cultures of fused cells secreting antibody of predefined specificity. Nature 1975; 256: 495-7.
2. Cauwenberghs N, Vanhoorelbeke K, Vauterin S, et al. Epitope mapping of inhibitory antibodies against platelet glycoprotein Ibalpha reveals interaction between the leucine-rich repeat N-terminal and C-terminal flanking domains of glycoprotein Ibalpha. Blood 2001; 98: 652-60.
3. Cauwenberghs N, Schlammadinger A, Vauterin S, et al. Fc-receptor dependent platelet aggregation induced by monoclonal antibodies against platelet glycoprotein Ib or von Willebrand factor. Thromb Haemost 2001; 85:679-85.
4. Huizinga EG, Tsuji S, Romijn RA, et al. Structures of glycoprotein Ibalpha and its complex with von Willebrand factor A1 domain. Science 2002; 297: 1176-9.
5. Uff S, Clemetson JM, Harrison T, et al. Crystal structure of the platelet glycoprotein Ibalpha N-terminal domain reveals an unmasking mechanism for receptor activation. J Biol Chem 2002; 277: 35657-63.
6. Cauwenberghs N, Meiring M, Vauterin S, et al. Antithrombotic effect of platelet glycoprotein Ib-blocking monoclonal antibody Fab fragments in non-human primates. Arterioscler Thromb Vasc Biol 2000; 20:1347-53.
7. Wu D, Meiring M, Kotze HE et al. Inhibition of platelet glycoprotein Ib, glycoprotein IIb/IIIa, or both by monoclonal antibodies prevents arterial thrombosis in baboons. Arterioscler Thromb Vasc Biol 2002; 22: 323-8.
8. Jaffers GJ, Fuller TC, Cosimi AB, et al. Monoclonal antibody therapy. Anti-idiotypic and non-anti-idiotypic antibodies to OKT3 arising despite intense immunosuppression. Transplantation 1986; 41: 572-8.
9. Bruggemann M, Winter G, Waldmann H, et al. The immunogenicity of chimeric antibodies. J Exp Med 1989; 170: 2153-7.
10. Morrison SL, Johnson MJ, Herzenberg LA, et al. Chimeric human-antibody molecules - Mouse antigen-binding domains with human constant region domains. Proe Nat Acad Sci USA 1984; 81: 6851-5.
11. Verhoeyen M, Milstein C, Winter G. Reshaping human antibodies: grafting an antilysozyme activity. Science 1988; 239: 1534-6.
12. Queen C, Schneider WP, Selick HE, et al. A humanized antibody that binds to the interleukin 2 receptor. Proc Natl Acad Sci USA 1989; 86: 10029-33.
13. Padlan EA. A possible procedure for reducing the immunogenicity of antibody variable domains while preserving their ligand-binding properties. Mol Immunol 1991; 28: 489-98.
14. Roguska MA, Pedersen JT, Keddy CA, et al. Humanization of murine monoclonal antibodies through variable domain resurfacing. Proc Natl Acad Sci USA 1994; 91: 969-73.
15. Roguska MA, Pedersen JT, Henry AH, et al. A comparison of two murine monoclonal antibodies humanized by CDR-grafting and variable domain resurfacing. Protein Eng 1996; 9: 895-904.
16. O'Connor SJ, Meng YG, Rezaie AR, et al. Humanization of an antibody against human protein C and calcium-dependence involving framework residues. Protein Eng 1998; 11: 321-8.
17. Orlandi R, Gussow DH, Jones PT, et al. Cloning immunoglobulin variable domains for expression by the polymerase chain reaction. Proc Natl Acad Sci USA 1989; 86: 3833-7.
18. Staelens S, Desmet J, Ngo TH, et al. Humanization by variable domain resurfacing and grafting on a human IgG4, using a new approach for determination of non-human like surface accessible framework residues based on homology modelling of variable domains. Mol Immunol 2006; 43: 1243-57.
19. Jacquemin M, Benhida A, Peerlinck K, et al. A human antibody directed to the factor VIII C1 domain inhibits factor VIII cofactor activity and binding to von Willebrand factor. Blood 2000; 95: 156-63.
20. Dewerchin M, Van der EL, Singh I, et al. Inhibition of factor VIII with a partially inhibitory human recombinant monoclonal antibody prevents thrombotic events in a transgenic model of type II HBS antithrombin deficiency in mice. J Thromb Haemost 2004; 2: 77-84.
21. Altschul SF, Madden TL, Schaffer AA, et al. Gapped BLAST and PSI-BLAST: a new generation of protein database search programs. Nucleic Acids Res 1997; 25: 3389-402.
22. Delhaise P, Bardiaux M, De Maeyer M, et al. The Brugel Package - Toward Computer-Aided-Design of Macromolecules. J Mol Graphics 1988; 6: 219-23.
23. Desmet J, Spriet J, Lasters I. Fast and accurate side-chain topology and energy refinement (FASTER) as a new method for protein structure optimization. Proteins 2002; 48: 31-43.
24. Vanhoorelbeke K, Pareyn I, Schlammadinger A, et al. Plasma glycocalicin as a source of GP1b alpha in the von Willebrand factor ristocetin cofactor ELISA. Thromb Haemost 2005; 93: 165-71.
25. Dubel S, Breitling F, Fuchs P, et al. Isolation of IgG antibody Fv-DNA from various mouse and rat hybridoma cell lines using the polymerase chain reaction with a simple set of primers. J Immunol Methods 1994; 175: 89-95.
26. Wang Z, Raifu M, Howard M, et al. Universal PCR amplification of mouse immunoglobulin gene variable regions: the design of degenerate primers and an assessment of the effect of DNA polymerase 3′ to 5′ exonuclease activity. J Immunol Methods 2000; 233: 167-77.
27. Kabat EA, Wu TT, Reid-Miller M, et al. Sequences of proteins of immunological interest 4th Ed. 1987.
28. Horton RM, Hunt HD, Ho SN, et al. Engineering hybrid genes without the use of restriction enzymes: gene splicing by overlap extension. Gene 1989; 77: 61-8.
29. Hagay Y, Lahav J, Levanon A, et al. Function-modulating human monoclonal antibodies against platelet-membrane receptors isolated from a phage-display library. J Thromb Haemost 2003; 1: 1829-36.
30. Ward CM, Andrews RK, Smith AI, et al. Mocarhagin, a novel cobra venom metalloproteinase, cleaves the platelet von Willebrand factor receptor glycoprotein Ibalpha. Identification of the sulfated tyrosine/anionic sequence Tyr-276-Glu-282 of glycoprotein Ibalpha as a binding site for von Willebrand factor and alpha-thrombin. Biochemistry 1996; 35: 4929-38.
31. Akiyama M, Takami H, Yoshida Y. The mechanism of cold-induced platelet aggregation in the presence of heparin. Tohoku J Exp Med 1995; 177: 365-74.
32. Cadroy Y, Hanson SR, Kelly AB, et al. Relative antithrombotic effects of monoclonal antibodies targeting different platelet glycoprotein-adhesive molecule interactions in nonhuman primates. Blood 1994; 83: 3218-24.
33. Becker BH, Miller JL. Effects of an antiplatelet glycoprotein Ib antibody on hemostatic function in the guinea pig. Blood 1989; 74: 690-4.
34. Luo D, Mah N, Krantz M, et al. V1-linker-Vh orientation-dependent expression of single chain Fv-containing an engineered disulfide-stabilized bond in the framework regions. J Biochem (Tokyo) 1995; 118: 825-31.
35. Kim JK, Min W, Lillehoj HS, et al. Generation and characterization of recombinant ScFv antibodies detecting Eimeria acervulina surface antigens. Hybridoma 2001; 20: 175-81.
36. Dai K, An G, Ruan C. Construction and characterization of bispecific single-chain antibody fragments SZ-2/SZ-21 against platelet glycoprotein Ib alpha and beta3. Zhonghua Yi Xue Za Zhi 2002; 82: 1493-7.