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Related Concept Videos

Phase II Conjugation Reactions: Overview01:14

Phase II Conjugation Reactions: Overview

Conjugation, a key component of phase II biotransformation reactions, is a vital process in drug detoxification. It involves transferring endogenous substances like glucuronic acid, sulfate, and glycine to drugs or their metabolites formed in phase I reactions. These conjugation reactions, often catalyzed by specific enzymes, transform potentially harmful metabolites into inactive, water-soluble forms easily excreted in urine or bile. By enhancing polarity and eliminating pharmacological...

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Related Experiment Video

Updated: Jul 9, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
08:47

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Published on: March 6, 2019

Modular Assembly of Bioconjugates Enabled by a Pyridine-Based Chemoselective Sequential Conjugation Platform.

Xiaobo Dang1, Chenyang Zhang1, Jinlong Shang1

  • 1Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China.

Angewandte Chemie (International Ed. in English)
|July 8, 2026
PubMed
Summary

This study introduces a new pyridine-based platform for site-selective bioconjugation, enabling stable, sequential coupling of amines and Cys residues. This method enhances therapeutic development by creating robust linkages for antibody-drug conjugates (ADCs).

Keywords:
antibody‐drug conjugates (ADCs)cysteine modificationsequential conjugation platformsite‐selective bioconjugationstable S‐aryl linkage

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Area of Science:

  • Chemical Biology
  • Medicinal Chemistry
  • Organic Synthesis

Background:

  • Site-selective cysteine (Cys) bioconjugation is crucial for developing chemical biology tools and therapeutics.
  • Existing methods for amine and Cys conjugation often result in unstable linkages, stereochemical issues, or limited versatility.
  • There is a need for robust and modular conjugation strategies for applications like antibody-drug conjugates (ADCs).

Purpose of the Study:

  • To develop a novel, programmable platform for chemoselective, sequential conjugation of alkylamines and Cys residues.
  • To create stable, non-chiral aryl-Cys linkages with high functional group tolerance and chemoselectivity.
  • To demonstrate the platform's utility in late-stage peptide modification, protein functionalization, and ADC construction.

Main Methods:

  • A pyridine-based scaffold was designed, incorporating a thianthrenium leaving group and a fluorine handle for sequential conjugation.
  • The platform was utilized for orthogonal coupling of alkylamines followed by Cys residues.
  • The method was applied to peptide diversification, protein modification, and the synthesis of a HER2-targeting ADC analog.

Main Results:

  • The developed platform enables sequential and orthogonal conjugation of alkylamines and Cys to form stable aryl-Cys linkages.
  • The conjugation process exhibits high chemoselectivity and broad functional group compatibility.
  • A HER2-targeting ADC analog (MRG002) was synthesized, demonstrating enhanced cytotoxicity and improved payload retention in serum.

Conclusions:

  • The pyridine-based conjugation platform offers a versatile and efficient approach for site-selective bioconjugation.
  • This strategy facilitates the development of advanced therapeutics, including ADCs with improved properties.
  • The platform enables modular assembly and late-stage functionalization for diverse bioconjugation applications.