Bispecific tandem diabody for tumor therapy with improved antigen binding and pharmacokinetics

Journal of Molecular Biology

Volumn 293, Issue 1, 1999, Pages 41-56

  Kipriyanov, Sergey M ^a   Moldenhauer, Gerhard ^a   Schuhmacher, Jochen ^a   Cochlovius, Björn ^a   Von Der Lieth, Claus Wilhelm ^a   Matys, E Ronald ^a   Little, Melvyn ^a  

^a GERMAN CANCER RESEARCH CENTER DKFZ   (Germany)

Author keywords

Bispecific diabody; Domain swapping; Human CD19; Human CD3; Tandem diabody

Indexed keywords

BISPECIFIC ANTIBODY; CD19 ANTIGEN; T LYMPHOCYTE ANTIGEN;

ANIMAL EXPERIMENT; ANTIGEN BINDING; AREA UNDER THE CURVE; ARTICLE; BACTERIAL GROWTH; BINDING AFFINITY; BINDING SITE; CANCER IMMUNOTHERAPY; CELL PROLIFERATION; CONTROLLED STUDY; CYTOLYSIS; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG STABILITY; ESCHERICHIA COLI; HUMAN; HUMAN CELL; INTRAVENOUS DRUG ADMINISTRATION; ISOTOPE LABELING; MALE; MOLECULAR WEIGHT; MOUSE; NONHUMAN; OPERON; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROMOTER REGION; TUMOR CELL;

ANIMALIA; BACTERIA (MICROORGANISMS); ESCHERICHIA COLI;

EID: 0033569478     PISSN: 00222836     EISSN: None     Source Type: Journal    
DOI: 10.1006/jmbi.1999.3156     Document Type: Article

References (65)

1. Adair J. R., Athwal D. S., Bodmer M., Bright S. M., Collins A., Pulito V. L., Rao P. E., Reedman R., Rothermel A. L., Xu D., Zivin R. A., Jolliffe L. K. Humanization of the murine anti-human CD3 monoclonal antibody OKT3. Human Antibodies Hybrid. 5:1994;41-47.
2. Adams G. P. Improving the tumor specificity and retention of antibody-based molecules. In Vivo. 12:1998;11-21.
3. Adams G. P., Schier R., Marshall K., Wolf E. J., McCall A. M., Marks J. D., Weiner L. M. Increased affinity leads to improved selective tumor delivery of single-chain Fv antibodies. Cancer Res. 58:1998;485-490.
4. Arakawa T., Timasheff S. N. The stabilization of proteins by osmolytes. Biophys. J. 47:1985;411-414.
5. Arndt K. M., Müller K. M., Plückthun A. Factors influencing the dimer to monomer transition of an antibody single-chain Fv fragment. Biochemistry. 37:1998;12918-12926.
6. Arndt M., Krauss J., Kipriyanov S. M., Pfreundschuh M., Little M. A bispecific diabody that mediates natural killer cell cytotoxicity against xenotransplanted human Hodgkin's tumors. Blood. 94:1999;2562-2568.
7. Bennett M. J., Choe S., Eisenberg D. Domain swapping: entangling alliances between proteins. Proc. Natl Acad. Sci. USA. 91:1994;3127-3131.
8. Blackwell J. R., Horgan R. A novel strategy for production of a highly expressed recombinant protein in an active form. FEBS Letters. 295:1991;10-12.
9. Bohlen H., Hopff T., Manzke O., Engert A., Kube D., Wickramanayake P. D., Diehl V., Tesch H. Lysis of malignant B cells from patients with B-chronic lymphocytic leukemia by autologous T cells activated with CD3×CD19 bispecific antibodies in combination with bivalent CD28 antibodies. Blood. 82:1993;1803-1812.
10. Bothmann H., Plückthun A. Selection for a periplasmic factor improving phage display and functional periplasmic expression. Nature Biotechnol. 16:1998;376-380.
11. Bowden G. A., Georgiou G. Folding and aggregation of beta-lactamase in the periplasmic space of Escherichia coli. J. Biol. Chem. 265:1990;16760-16766.
12. Brennan M., Davidson P. F., Paulus H. Preparation of bispecific antibodies by chemical recombination of monoclonal immunoglobulin G1 fragments. Science. 229:1985;81-83.
13. Carter P., Ridgway J., Zhu Z. Toward the production of bispecific antibody fragments for clinical applications. J. Hematother. 4:1995;463-470.
14. Casey J. L., Keep P. A., Chester K. A., Robson L., Hawkins R. E., Begent R. H. Purification of bacterially expressed single chain Fv antibodies for clinical applications using metal chelate chromatography. J. Immunol. Methods. 179:1995;105-116.
15. Coloma M. J., Morrison S. L. Design and production of novel tetravalent bispecific antibodies. Nature Biotechnol. 15:1997;159-163.
16. de Kruif J., Logtenberg T. Leucine zipper dimerized bivalent and bispecific scFv antibodies from a semi-synthetic antibody phage display library. J. Biol. Chem. 271:1996;7630-7634.
17. Fanger M. W., Morganelli P. M., Guyre P. M. Bispecific antibodies. Crit. Rev. Immunol. 12:1992;101-124.
18. FitzGerald K., Holliger P., Winter G. Improved tumour targeting by disulphide stabilized diabodies expressed in Pichia pastoris. Protein Eng. 10:1997;1221-1225.
19. Gill S. C., von Hippel P. H. Calculation of protein extinction coefficients from amino acid sequence data. Anal. Biochem. 182:1989;319-326.
20. Givol D. The minimal antigen-binding fragment of antibodies-Fv fragment. Mol. Immunol. 28:1991;1379-1386.
21. 2antibody containing thioether-linked Fab′γ fragments. J. Immunol. 139:1987;2367-2375.
22. Glockshuber R., Malia M., Pfitzinger I., Plückthun A. A comparison of strategies to stabilize immunoglobulin Fv-fragments. Biochemistry. 29:1990;1362-1367.
23. Gruber M., Schodin B. A., Wilson E. R., Kranz D. M. Efficient tumor cell lysis mediated by a bispecific single chain antibody expressed in Escherichia coli. J. Immunol. 152:1994;5368-5374.
24. Harris L. J., Skaletsky E., McPherson A. Crystallographic structure of an intact IgG1 monoclonal antibody. J. Mol. Biol. 275:1998;861-872.
25. Holck A., Kleppe K. Cloning and sequencing of the gene for the DNA-binding 17 K protein of Escherichia coli. Gene. 67:1988;117-124.
26. Holliger P., Prospero T., Winter G. "Diabodies": small bivalent and bispecific antibody fragments. Proc. Natl Acad. Sci. USA. 90:1993;6444-6448.
27. Holliger P., Brissinck J., Williams R. L., Thielemans K., Winter G. Specific killing of lymphoma cells by cytotoxic T-cells mediated by a bispecific diabody. Protein Eng. 9:1996;299-305.
28. Horn U., Strittmatter W., Krebber A., Knupfer U., Kujau M., Wenderoth R., Müller K., Matzku S., Plückthun A., Riesenberg D. High volumetric yields of functional dimeric miniantibodies in Escherichia coli, using an optimized expression vector and high-cell-density fermentation under non-limited growth conditions. Appl. Microbiol. Biotechnol. 46:1996;524-532.
29. Huston J. S., Levinson D., Mudgett Hunter M., Tai M. S., Novotny J., Margolies M. N., Ridge R. J., Bruccoleri R. E., Haber E., Crea R., Oppermann H. Protein engineering of antibody binding sites: recovery of specific activity in an anti-digoxin single-chain Fv analogue produced in Escherichia coli. Proc. Natl Acad. Sci. USA. 85:1988;5879-5883.
30. Khazaeli M. B., Conry R. M., LoBuglio A. F. Human immune response to monoclonal antibodies. J. Immunother. 15:1994;42-52.
31. Kipriyanov S. M., Dübel S., Breitling F., Kontermann R. E., Little M. Recombinant single-chain Fv fragments carrying C-terminal cysteine residues: production of bivalent and biotinylated miniantibodies. Mol. Immunol. 31:1994;1047-1058.
32. Kipriyanov S. M., Kupriyanova O. A., Little M., Moldenhauer G. Rapid detection of recombinant antibody fragments directed against cell-surface antigens by flow cytometry. J. Immunol. Methods. 196:1996a;51-62.
33. Kipriyanov S. M., Little M., Kropshofer H., Breitling F., Gotter S., Dübel S. Affinity enhancement of a recombinant antibody: formation of complexes with multiple valency by a single-chain Fv fragment-core streptavidin fusion. Protein Eng. 9:1996b;203-211.
34. Kipriyanov S. M., Moldenhauer G., Little M. High level production of soluble single chain antibodies in small-scale Escherichia coli cultures. J. Immunol. Methods. 200:1997a;69-77.
35. Kipriyanov S. M., Moldenhauer G., Martin A. C., Kupriyanova O. A., Little M. Two amino acid mutations in an anti-human CD3 single chain Fv antibody fragment that affect the yield on bacterial secretion but not the affinity. Protein Eng. 10:1997b;445-453.
36. Kipriyanov S. M., Moldenhauer G., Strauss G., Little M. Bispecific CD3×CD19 diabody for T cell-mediated lysis of malignant human B cells. Int. J. Cancer. 77:1998;763-772.
37. Kung P. C., Golstein G., Reinherz E. L., Schlossman S. F. Monoclonal antibodies defining distinctive human T cell surface antigens. Science. 206:1979;347-349.
38. Kurucz I., Titus J. A., Jost C. R., Jacobus C. M., Segal D. M. Retargeting of CTL by an efficiently refolded bispecific single-chain Fv dimer produced in bacteria. J. Immunol. 154:1995;4576-4582.
39. Lee J. C., Timasheff S. N. The stabilization of proteins by sucrose. J. Biol. Chem. 256:1981;7193-7201.
40. Le Gall F., Kipriyanov S. M., Moldenhauer G., Little M. Di-, tri- and tetrameric single chain Fv antibody fragments against human CD19: effect of valency on cell binding. FEBS Letters. 453:1999;164-168.
41. Mallender W. D., Carrero J., Voss E. Comparative properties of the single chain antibody and Fv derivatives of mAb 4-4-20. Relationship between interdomain interactions and the high affinity for fluorescein ligand. J. Biol. Chem. 271:1996;5338-5346.
42. Matzinger P. The JAM test. A simple assay for DNA fragmentation and cell death. J. Immunol. Methods. 145:1991;185-192.
43. R3 and autogenous negative control by repressor. J. Mol. Biol. 139:1980;147-161.
44. Müller K. M., Arndt K. M., Bauer K., Plückthun A. Tandem immobilized metal-ion affinity chromatography/immunoaffinity purification of His-tagged proteins-evaluation of two anti-His-tag monoclonal antibodies. Anal. Biochem. 259:1998a;54-61.
45. Müller K. M., Arndt K. M., Plückthun A. A dimeric bispecific miniantibody combines two specificities with avidity. FEBS Letters. 432:1998b;45-49.
46. L) of an antibody used as heterodimerization domain for bispecific miniantibodies. FEBS Letters. 422:1998c;259-264.
47. Nieba L., Honegger A., Krebber C., Pluckthun A. Disrupting the hydrophobic patches at the antibody variable/constant domain interface: improved in vivo folding and physical characterization of an engineered scFv fragment. Protein Eng. 10:1997;435-444.
48. Perisic O., Webb P. A., Holliger P., Winter G., Williams R. L. Crystal structure of a diabody, a bivalent antibody fragment. Structure. 2:1994;1217-1226.
49. Pezzutto A., Dörken B., Rabinovitch P. S., Ledbetter J. A., Moldenhauer G., Clark E. A. CD19 monoclonal antibody HD37 inhibits anti-immunoglobulin-induced B cell activation and proliferation. J. Immunol. 138:1987;2793-2799.
50. Plückthun A., Pack P. New protein engineering approaches to multivalent and bispecific antibody fragments. Immunotechnology. 3:1997;83-105.
51. Polymenis M., Stollar B. D. Domain interactions and antigen binding of recombinant anti-Z-DNA antibody variable domains. The role of heavy and light chains measured by surface plasmon resonance. J. Immunol. 154:1995;2198-2208.
52. Ridder R., Schmitz R., Legay F., Gram H. Generation of rabbit monoclonal antibody fragments from a combinatorial phage display library and their production in the yeast Pichia pastoris. Bio/Technology. 13:1995;255-260.
53. Rodriguez R., Chinea G., Lopez N., Pons T., Vriend G. Homology modeling, model and software evaluation: three related resources. Bioinformatics. 14:1998;523-528.
54. Sanger F., Nicklen S., Coulson A. R. DNA sequencing with chain-terminating inhibitors. Proc. Natl Acad. Sci. USA. 74:1977;5463-5467.
55. Sawyer J. R., Schlom J., Kashmiri S. V. S. The effect of induction conditions on production of a soluble anti-tumor sFv in Escherichia coli. Protein Eng. 7:1994;1401-1406.
56. Schlunegger M. P., Bennett M. J., Eisenberg D. Oligomer formation by 3D domain swapping: a model for protein assembly and misassembly. Advan. Protein Chem. 50:1997;61-122.
57. Schodin B. A., Kranz D. M. Binding affinity and inhibitory properties of a single-chain anti-T cell receptor antibody. J. Biol. Chem. 268:1993;25722-25727.
58. Schulze R. A., Kontermann R. E., Queitsch I., Dübel S., Bautz E. K. Thiophilic adsorption chromatography of recombinant single-chain antibody fragments. Anal. Biochem. 220:1994;212-214.
59. Shusta E. V., Raines R. T., Plückthun A., Wittrup K. D. Increasing the secretory capacity of Saccharomyces cerevisiae for production of single-chain antibody fragments. Nature Biotechnol. 16:1998;773-777.
60. Thisted T., Sorensen N. S., Wagner E. G., Gerdes K. Mechanism of post-segregational killing: Sok antisense RNA interacts with Hok mRNA via its 5′-end single-stranded leader and competes with the 3′-end of Hok mRNA for binding to the mok translational initiation region. EMBO J. 13:1994;1960-1968.
61. Tsumoto K., Shinoki K., Kondo H., Uchikawa M., Juji T., Kumagai I. Highly efficient recovery of functional single-chain Fv fragments from inclusion bodies overexpressed in Escherichia coli by controlled introduction of oxidizing reagent-application to a human single-chain Fv fragment. J. Immunol. Methods. 219:1998;119-129.
62. Uckun F. M., Ledbetter J. A. Immunobiologic differences between normal and leukemic human B-cell precursors. Proc. Natl Acad. Sci. USA. 85:1988;8603-8607.
63. Xie G., Timasheff S. N. Mechanism of the stabilization of ribonuclease A by sorbitol: preferential hydration is greater for the denatured then for the native protein. Protein Sci. 6:1997;211-221.
64. Zhu Z., Zapata G., Shalaby R., Snedecor B., Chen H., Carter P. High level secretion of a humanized bispecific diabody from Escherichia coli. Bio/Technology. 14:1996;192-196.
65. Zhu Z., Presta L. G., Zapata G., Carter P. Remodeling domain interfaces to enhance heterodimer formation. Protein Sci. 6:1997;781-788.