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Site-Selective Antibody-Drug Conjugation Chemistry based on Inverse-electron- demand Diels-Alder Reaction

목차

1. Introduction 1
1.1 Antibody-drug conjugate (ADC) 1
1.2 Importance of site selective drug conjugation to antibody 2
1.3 Site selective conjugation technology using click-to-release chemistry 4
1.4 Aim of thesis 6
2. Results and Discussion 7
2.1 Synthesis of peptide TCO NHS ester linker 7
2.2 Antibody-peptide conjugation 11
2.3 Drug conjugation by 'click to release' 15
3. Conclusion 18
4. Experimental Section 19
4.1 General information 19
4.2 Synthetic procedure 20
4.3 Protocols to produce ADC 33
5. References 34
6. Analytical results 36
6.1 HPLC chromatograms of antibody-peptide conjugates 36
6.2 1H NMR and 13C NMR spectra 46

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