Antibody-Drug Conjugates: Basic Concepts and Structures

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Antibody-Drug Conjugates and Cellular Metabolic Dynamics

Abstract

Antibody-drug conjugates (ADCs) are new modality of anticancer therapeutics. To enhance the translation, three components of an ADC drug—antibody, linker, and cytotoxin— need to be carefully optimized. The selection of antibody and target plays a key role in the success of ADCs. Ideal targets are the antigens which are expressed only on tumor cells. As one of crucial component, linkers such as cleavable linkers and noncleavable linkers have been explored. Finally, the highly effective payloads including tubulin inhibitors and DNA-damaging antibiotics have been discussed.

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References

  1. Thomas A, Teicher BA, Hassan R. Antibody-drug conjugates for cancer therapy. Lancet Oncol. 2016;17(6):e254–62. https://doi.org/10.1016/S1470-2045(16)30030-4.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  2. Lin L, Ding Q, Tang Q, et al. Antibody-drug conjugates and their application in the treatment of hematological malignancies. Acta Pharm Sin. 2012;47(10):1287–96.

    CAS  Google Scholar 

  3. Jen EY, Ko CW, Lee JE, et al. FDA approval: Gemtuzumab ozogamicin for the treatment of adults with newly-diagnosed CD33-positive acute myeloid leukemia. Clin Cancer Res. 2018;24:3242. https://doi.org/10.1158/1078-0432.CCR-17-3179.

    Article  CAS  PubMed  Google Scholar 

  4. Pan LQ, Wang HB, **e ZM, et al. Novel conjugation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) with monomethyl auristatin E for efficient antitumor drug delivery. Adv Mater. 2013;25(34):4718–22.

    Article  CAS  PubMed  Google Scholar 

  5. Polson AG, Calemine-Fenaux J, Chan P, et al. Antibody-drug conjugates for the treatment of non-Hodgkin’s lymphoma: target and linker-drug selection. Cancer Res. 2009;69:2358–64.

    Article  CAS  PubMed  Google Scholar 

  6. Lewis-Phillips GD, Li G, Dugger DL. Targeting HER2-postive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008;6:9280–90.

    Article  Google Scholar 

  7. Barriuso B, Antolín P, Arias FJ, et al. Anti-human endoglin (hCD105) immunotoxin— containing recombinant single chain ribosome-inactivating protein musarmin 1. Toxins. 2016;8(6):184.

    Article  PubMed  PubMed Central  Google Scholar 

  8. Kalim M, Chen J, Wang S, et al. Intracellular trafficking of new anticancer therapeutics: antibody-drug conjugates. Drug Des Devel Ther. 2017;11:2265–76.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  9. Tsuchikama K, An ZQ. Antibody-drug conjugates: recent advances in conjugation and linker chemistries. Protein Cell. 2018;9(1):33–46.

    Article  CAS  PubMed  Google Scholar 

  10. Jain N, Smith SW, Ghone S, et al. Current ADC linker chemistry. Pharm Res. 2015;32:3526–40.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  11. Lai J, Wang Y, Wu S, et al. Elimination of melanoma by sortase A generated TCR like antibody-drug conjugates (TL-ADCs) targeting intracellular melanoma antigen MART-1. Biomaterials. 2018;178:158–69.

    Article  CAS  PubMed  Google Scholar 

  12. Axup JY, Bajjuri KM, Ritland M, et al. Synthesis of site-specific antibody-drug conjugates using unnatural amino acids. Proc Natl Acad Sci USA. 2012;109:16101–6.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  13. Zhu GD, Fu YX. Design of next generation antibody drug conjugates. Acta Pharm Sin. 2013;48(7):1053–70.

    CAS  Google Scholar 

  14. Chudasama V, Maruani A, Caddick S. Recent advances in the construction of antibody-drug conjugates. Nat Chem. 2016;8:114–9.

    Article  CAS  PubMed  Google Scholar 

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Correspondence to **biao Zhan .

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Zhan, J. (2023). Antibody-Drug Conjugates: Basic Concepts and Structures. In: Chen, S., Zhan, J. (eds) Antibody-Drug Conjugates and Cellular Metabolic Dynamics. Springer, Singapore. https://doi.org/10.1007/978-981-19-5638-6_1

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