An engineered affibody molecule with pH-dependent binding to FcRN mediates extended circulatory half-life of a fusion protein

Proceedings of the National Academy of Sciences of the United States of America

Volumn 111, Issue 48, 2014, Pages 17110-17115

  Seijsing, Johan ^a   Lindborg, Malin ^b   Höidén Guthenberg, Ingmarie ^b   Bönisch, Heiko ^b   Guneriusson, Elin ^b   Frejd, Fredrik Y ^b,c   Abrahmsén, Lars ^b,d   Ekblad, Caroline ^b   Löfblom, John ^a   Uhlén, Mathias ^a   Gräslund, Torbjörn ^a  

^a ROYAL INSTITUTE OF TECHNOLOGY   (Sweden)

^b Affibody AB   (Sweden)

^c UPPSALA UNIVERSITY   (Sweden)

^d KAROLINSKA INSTITUTE   (Sweden)

Author keywords

ABD; Affibody molecule; Albumin binding domain; Fc receptor; Neonatal; Pharmacokinetics

Indexed keywords

FC RECEPTOR; HYBRID PROTEIN; NEONATAL FC RECEPTOR; RECOMBINANT PROTEIN; UNCLASSIFIED DRUG; CARRIER PROTEIN; FC RECEPTOR, NEONATAL; HLA ANTIGEN CLASS 1; PEPTIDE LIBRARY; PROTEIN BINDING;

AFFIBODY MOLECULE; ANIMAL CELL; ARTICLE; BIOPHYSICS; CONTROLLED STUDY; HUMAN; HUMAN CELL; IN VITRO STUDY; MOLECULE; MOUSE; NONHUMAN; PH; PHAGE DISPLAY; PLASMA HALF LIFE; ANIMAL; BINDING COMPETITION; BLOOD; ENZYME LINKED IMMUNOSORBENT ASSAY; FLOW CYTOMETRY; GENETICS; HALF LIFE TIME; HELA CELL LINE; INBRED MOUSE STRAIN; MALE; METABOLISM; PEPTIDE LIBRARY; TUMOR CELL LINE;

MUS;

ANIMALS; BINDING, COMPETITIVE; CARRIER PROTEINS; CELL LINE, TUMOR; ENZYME-LINKED IMMUNOSORBENT ASSAY; FLOW CYTOMETRY; HALF-LIFE; HELA CELLS; HISTOCOMPATIBILITY ANTIGENS CLASS I; HUMANS; HYDROGEN-ION CONCENTRATION; MALE; MICE, INBRED STRAINS; PEPTIDE LIBRARY; PROTEIN BINDING; RECEPTORS, FC; RECOMBINANT FUSION PROTEINS;

EID: 84915818878     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1417717111     Document Type: Article

References (37)

1. Beck A, Reichert JM (2011) Therapeutic Fc-fusion proteins and peptides as successful alternatives to antibodies. MAbs 3(5):415-416.
2. Kontermann RE (2011) Strategies for extended serum half-life of protein therapeutics. Curr Opin Biotechnol 22(6):868-876.
3. Yamaoka T, Tabata Y, Ikada Y (1994) Distribution and tissue uptake of poly(ethylene glycol) with different molecular weights after intravenous administration to mice. J Pharm Sci 83(4):601-606.
4. Caliceti P, Veronese FM (2003) Pharmacokinetic and biodistribution properties of poly (ethylene glycol)-protein conjugates. Adv Drug Deliv Rev 55(10):1261-1277.
5. Alconcel SNS, Baas AS, Maynard HD (2011) FDA-approved poly(ethylene glycol)-protein conjugate drugs. Polym Chem 2:1442-1448.
6. Andersen JT, et al. (2012) Structure-based mutagenesis reveals the albumin-binding site of the neonatal Fc receptor. Nat Commun 3:610.
7. Roopenian DC, Akilesh S (2007) FcRn: The neonatal Fc receptor comes of age. Nat Rev Immunol 7(9):715-725.
8. Brambell FW (1966) The transmission of immunity from mother to young and the catabolism of immunoglobulins. Lancet 2(7473):1087-1093.
9. Brambell FW, Hemmings WA, Morris IG (1964) A theoretical model of gammaglobulin catabolism. Nature 203:1352-1354.
10. Junghans RP, Anderson CL (1996) The protection receptor for IgG catabolism is the beta2-microglobulin-containing neonatal intestinal transport receptor. Proc Natl Acad Sci USA 93(11):5512-5516.
11. Andersen JT, Sandlie I (2009) The versatile MHC class I-related FcRn protects IgG and albumin from degradation: Implications for development of new diagnostics and therapeutics. Drug Metab Pharmacokinet 24(4):318-332.
12. Raghavan M, Gastinel LN, Bjorkman PJ (1993) The class I major histocompatibility complex related Fc receptor shows pH-dependent stability differences correlating with immunoglobulin binding and release. Biochemistry 32(33):8654-8660.
13. Chuang VTG, Kragh-Hansen U, Otagiri M (2002) Pharmaceutical strategies utilizing recombinant human serum albumin. Pharm Res 19(5):569-577.
14. Stork R, Campigna E, Robert B, Müller D, Kontermann RE (2009) Biodistribution of a bispecific single-chain diabody and its half-life extended derivatives. J Biol Chem 284(38):25612-25619.
15. Czajkowsky DM, Hu J, Shao Z, Pleass RJ (2012) Fc-fusion proteins: New developments and future perspectives. EMBO Mol Med 4(10):1015-1028.
16. Makrides SC, et al. (1996) Extended in vivo half-life of human soluble complement receptor type 1 fused to a serum albumin-binding receptor. J Pharmacol Exp Ther 277(1):534-542.
17. Nygren P-A (2008) Alternative binding proteins: Affibody binding proteins developed from a small three-helix bundle scaffold. FEBS J 275(11):2668-2676.
18. Löfblom J, et al. (2010) Affibody molecules: Engineered proteins for therapeutic, diagnostic and biotechnological applications. FEBS Lett 584(12):2670-2680.
19. Baum RP, et al. (2010) Molecular imaging of HER2-expressing malignant tumors in breast cancer patients using synthetic 111In- or 68Ga-labeled affibody molecules. J Nucl Med 51(6):892-897.
20. Seijsing J, Lindborg M, Löfblom J, Uhlén M, Gräslund T (2013) Robust expression of the human neonatal Fc receptor in a truncated soluble form and as a full-length membrane-bound protein in fusion with eGFP. PLoS ONE 8(11):e81350.
21. Nord K, et al. (1997) Binding proteins selected from combinatorial libraries of an alpha-helical bacterial receptor domain. Nat Biotechnol 15(8):772-777.
22. Grönwall C, et al. (2007) Selection and characterization of Affibody ligands binding to Alzheimer amyloid beta peptides. J Biotechnol 128(1):162-183.
23. Jonsson A, Dogan J, Herne N, Abrahmsén L, Nygren P-A (2008) Engineering of a femtomolar affinity binding protein to human serum albumin. Protein Eng Des Sel 21(8):515-527.
24. Frejd F (2012) in Therapeutic Proteins: Strategies to Modulate Their Plasma Half-Lives, ed Kontermann R (Wiley-Blackwell, Hoboken, NJ), pp 269-283.
25. Hopp J, et al. (2010) The effects of affinity and valency of an albumin-binding domain (ABD) on the half-life of a single-chain diabody-ABD fusion protein. Protein Eng Des Sel 23(11):827-834.
26. Orlova A, et al. (2013) Site-specific radiometal labeling and improved biodistribution using ABY-027, a novel HER2-targeting affibody molecule albumin-binding domain fusion protein. J Nucl Med 54(6):961-968.
27. Mezo AR, et al. (2008) Reduction of IgG in nonhuman primates by a peptide antagonist of the neonatal Fc receptor FcRn. Proc Natl Acad Sci USA 105(7):2337-2342.
28. Kim J, et al. (2006) Albumin turnover: FcRn-mediated recycling saves as much albumin from degradation as the liver produces. Am J Physiol Gastrointest Liver Physiol 290(2): G352-G360.
29. Hinton PR, et al. (2004) Engineered human IgG antibodies with longer serum halflives in primates. J Biol Chem 279(8):6213-6216.
30. Petkova SB, et al. (2006) Enhanced half-life of genetically engineered human IgG1 antibodies in a humanized FcRn mouse model: Potential application in humorally mediated autoimmune disease. Int Immunol 18(12):1759-1769.
31. Zalevsky J, et al. (2010) Enhanced antibody half-life improves in vivo activity. Nat Biotechnol 28(2):157-159.
32. Gurbaxani B, Dela Cruz LL, Chintalacharuvu K, Morrison SL (2006) Analysis of a family of antibodies with different half-lives in mice fails to find a correlation between affinity for FcRn and serum half-life. Mol Immunol 43(9):1462-1473.
33. Datta-Mannan A, et al. (2012) FcRn affinity-pharmacokinetic relationship of five human IgG4 antibodies engineered for improved in vitro FcRn binding properties in cynomolgus monkeys. Drug Metab Dispos 40(8):1545-1555.
34. Andersen JT, Dee Qian J, Sandlie I (2006) The conserved histidine 166 residue of the human neonatal Fc receptor heavy chain is critical for the pH-dependent binding to albumin. Eur J Immunol 36(11):3044-3051.
35. Medesan C, Matesoi D, Radu C, Ghetie V, Ward ES (1997) Delineation of the amino acid residues involved in transcytosis and catabolism of mouse IgG1. J Immunol 158(5):2211-2217.
36. Orlova A, et al. (2006) Tumor imaging using a picomolar affinity HER2 binding affibody molecule. Cancer Res 66(8):4339-4348.
37. Gunneriusson E, Nord K, Uhlén M, Nygren P (1999) Affinity maturation of a Taq DNA polymerase-specific affibody by helix shuffling. Protein Eng 12(10):873-878.