4.7 Article

Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)

Journal

CHEMICAL COMMUNICATIONS
Volume 51, Issue 53, Pages 10624-10627

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c5cc03557k

Keywords

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Funding

  1. Cancer Research UK
  2. Engineering and Physical Sciences Research Council (EPSRC)
  3. BBSRC
  4. BRC
  5. Wellcome Trust
  6. HEFCE
  7. SBC
  8. MRC
  9. UCL
  10. UCLB
  11. CCIC collaboration - CRUK & EPSRC Comprehensive Cancer Imaging Centre at KCL UCL
  12. Biotechnology and Biological Sciences Research Council [BB/L024349/1] Funding Source: researchfish
  13. Cancer Research UK [21030, 16463] Funding Source: researchfish
  14. Medical Research Council [G1001497, MC_PC_12024] Funding Source: researchfish
  15. BBSRC [BB/L024349/1] Funding Source: UKRI
  16. MRC [G1001497, MC_PC_12024] Funding Source: UKRI

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Herein we report the use of next generation maleimides (NGMs) for the construction of a potent antibody-drug conjugate (ADC) via functional disulfide bridging. The linker has excellent stability in blood serum and the ADC, armed with monomethyl auristatin E (MMAE), shows excellent potency and cancer cell selectivity in vitro.

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