A general approach to site-specific antibody drug conjugates

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

Volumn 111, Issue 5, 2014, Pages 1766-1771

  Tian, Feng ^a   Lu, Yingchun ^a   Manibusan, Anthony ^a   Sellers, Aaron ^a   Tran, Hon ^a,f   Sun, Ying ^a   Phuong, Trung ^a   Barnett, Richard ^a   Hehli, Brad ^a   Song, Frank ^a   DeGuzman, Michael J ^b   Ensari, Semsi ^b,g   Pinkstaff, Jason K ^c   Sullivan, Lorraine M ^c   Biroc, Sandra L ^c   Cho, Ho ^a   Schultz, Peter G ^d   Di Joseph, John ^e   Dougher, Maureen ^e   Ma, Dangshe ^e   Dushin, Russell ^e   Leal, Mauricio ^e   Tchistiakova, Lioudmila ^e   Feyfant, Eric ^e,h   Gerber, Hans Peter ^e   Sapra, Puja ^e   more..

^a AMBRX INC   (United States)

^b CMC Department   (United States)

^c Ambrx   (United States)

^d SCRIPPS RESEARCH INSTITUTE   (United States)

^e PFIZER INC   (United States)

^f ELI LILLY AND COMPANY   (United States)

^g GENENTECH INC   (United States)

^h SCHRÖDINGER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACID; ANTIBODY CONJUGATE; ANTIBODY DRUG CONJUGATE; CYSTEINE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; GENOMIC DNA; GLYCOPROTEIN; GREEN FLUORESCENT PROTEIN; HYDROXYLAMINE; KETONE; MEMBRANE ANTIGEN; MONOMETHYL AURISTATIN D; OXIME; PROTEIN INHIBITOR; PROTEINASE; TRANSFER RNA; TRASTUZUMAB; TUBULIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBODY TITER; ANTINEOPLASTIC ACTIVITY; ARTICLE; BATCH CELL CULTURE; CANCER CELL CULTURE; CANCER IMMUNOTHERAPY; CELL VIABILITY; CHEMICAL MODIFICATION; CHO CELL; CONTROLLED STUDY; DISULFIDE BOND; DOSE RESPONSE; DRUG CONJUGATION; FED BATCH CULTURE; GENE EXPRESSION; GENETIC CODE; HALF LIFE TIME; HEAVY CHAIN; LIGHT CHAIN; LIQUID CHROMATOGRAPHY; MAMMAL CELL; NONHUMAN; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SINGLE DRUG DOSE; SYNTHESIS; TANDEM MASS SPECTROMETRY; TUMOR MODEL; TUMOR XENOGRAFT;

ANIMALS; ANTIBODIES; BATCH CELL CULTURE TECHNIQUES; CELL DEATH; CELL LINE; CHO CELLS; CRICETINAE; CRICETULUS; CYSTEINE; HUMANS; IMMUNOCONJUGATES; PHARMACEUTICAL PREPARATIONS; PROTEIN ENGINEERING; PROTEIN STABILITY; RATS;

EID: 84893452692     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1321237111     Document Type: Article

References (31)

1. Sapra P, Hooper AT, O'Donnell CJ, Gerber H-P (2011) Investigational antibody drug conjugates for solid tumors. Expert Opin Investig Drugs 20(8):1131-1149.
2. Wu AM, Senter PD (2005) Arming antibodies: Prospects and challenges for immunoconjugates. Nat Biotechnol 23(9):1137-1146.
3. Polakis P (2005) Arming antibodies for cancer therapy. Curr Opin Pharmacol 5(4): 382-387.
4. Carter PJ, Senter PD (2008) Antibody-drug conjugates for cancer therapy. Cancer J 14(3):154-169.
5. Hamblett KJ, et al. (2004) Effects of drug loading on the antitumor activity of a monoclonal antibody drug conjugate. Clin Cancer Res 10(20):7063-7070.
6. Junutula JR, et al. (2008) Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index. Nat Biotechnol 26(8):925-932.
7. Jeffrey SC, et al. (2013) A potent anti-CD70 antibody-drug conjugate combining a dimeric pyrrolobenzodiazepine drug with site-specific conjugation technology. Bioconjug Chem 24(7):1256-1263.
8. Strop P, et al. (2013) Location matters: Site of conjugation modulates stability and pharmacokinetics of antibody drug conjugates. Chem Biol 20(2):161-167.
9. Axup JY, et al. (2012) Synthesis of site-specific antibody-drug conjugates using unnatural amino acids. Proc Natl Acad Sci USA 109(40):16101-16106.
10. Cho H, et al. (2011) Optimized clinical performance of growth hormone with an expanded genetic code. Proc Natl Acad Sci USA 108(22):9060-9065.
11. Mukai T, et al. (2008) Adding l-lysine derivatives to the genetic code of mammalian cells with engineered pyrrolysyl-tRNA synthetases. Biochem Biophys Res Commun 371(4):818-822.
12. Ou W, et al. (2011) Site-specific protein modifications through pyrroline-carboxylysine residues. Proc Natl Acad Sci USA 108(26):10437-10442.
13. Verdier-Pinard P, Kepler JA, Pettit GR, Hamel E (2000) Sustained intracellular retention of dolastatin 10 causes its potent antimitotic activity. Mol Pharmacol 57(1):180-187.
14. Damelin M, et al. (2011) Delineation of a cellular hierarchy in lung cancer reveals an oncofetal antigen expressed on tumor-initiating cells. Cancer Res 71(12):4236-4246.
15. Lewis Phillips GD, et al. (2008) Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res 68(22):9280-9290.
16. Köhrer C, Sullivan EL, RajBhandary UL (2004) Complete set of orthogonal 21st aminoacyl-tRNA synthetase-amber, ochre and opal suppressor tRNA pairs: Concomitant suppression of three different termination codons in an mRNA in mammalian cells. Nucleic Acids Res 32(21):6200-6211.
17. Chin J, et al. (2003) An expended eukaryotic genetic code. Science 301:964-967.
18. Xie J, Schultz PG (2005) Adding amino acids to the genetic repertoire. Curr Opin Chem Biol 9(6):548-554.
19. Xu X, et al. (2011) The genomic sequence of the Chinese hamster ovary (CHO)-K1 cell line. Nat Biotechnol 29(8):735-741.
20. Tian F, Norman T, Chu S (2006) Hybrid suppressor tRNA for vertebrate cells. Patent publication number US20100159586.
21. Wurm FM (2004) Production of recombinant protein therapeutics in cultivated mammalian cells. Nat Biotechnol 22(11):1393-1398.
22. Jewett JC, Bertozzi CR (2010) Cu-free click cycloaddition reactions in chemical biology. Chem Soc Rev 39(4):1272-1279.
23. Doronina SO, et al. (2003) Development of potent monoclonal antibody auristatin conjugates for cancer therapy. Nat Biotechnol 21(7):778-784.
24. Liu C, et al. (1996) Eradication of large colon tumor xenografts by targeted delivery of maytansinoids. Proc Natl Acad Sci USA 93(16):8618-8623.
25. Sapra P, et al. (2013) Long-term tumor regression induced by an antibody-drug conjugate that targets 5T4, an oncofetal antigen expressed on tumor-initiating cells. Mol Cancer Ther 12(1):38-47.
26. Shen B-Q, et al. (2012) Conjugation site modulates the in vivo stability and therapeutic activity of antibody-drug conjugates. Nat Biotechnol 30(2):184-189.
27. Polson AG, et al. (2009) Antibody-drug conjugates for the treatment of non-Hodgkin's lymphoma: Target and linker-drug selection. Cancer Res 69(6):2358-2364.
28. Alley SC, et al. (2008) Contribution of linker stability to the activities of anticancer immunoconjugates. Bioconjug Chem 19(3):759-765.
29. Ducry L, Stump B (2010) Antibody-drug conjugates: Linking cytotoxic payloads to monoclonal antibodies. Bioconjug Chem 21(1):5-13.
30. Junutula JR, et al. (2010) Engineered thio-trastuzumab-DM1 conjugate with an improved therapeutic index to target human epidermal growth factor receptor 2-positive breast cancer. Clin Cancer Res 16(19):4769-4778.
31. Burris HA, 3rd, et al. (2011) Phase II study of the antibody drug conjugate trastuzumab-DM1 for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer after prior HER2-directed therapy. J Clin Oncol 29(4):398-405.