Related Experiment Video
Updated: May 15, 2026

09:14
Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
Published on: July 20, 2016
Antibody-Drug Conjugates Synthesis Using Maleimide Chemistry
Camille Martin1, Sreenivasachary Nampally2
1AC Immune SA, Chemistry Department, EPFL Innovation Park, Lausanne, Switzerland. camille.martin@acimmune.com.
Methods in Molecular Biology (Clifton, N.J.)
|May 13, 2026
Summary
Antibody-drug conjugates (ADCs) are created by linking small molecules to antibodies. This study details the bioconjugation of a vedotin linker-payload to immunoglobulin G (IgG) and analyzes the resulting ADC for targeted drug delivery.
Area of Science:
- Bioconjugation Chemistry
- Antibody-Drug Conjugate Development
- Molecular Targeting
Background:
- Monoclonal antibodies (mAbs) are crucial for targeted therapies.
- Bioconjugation enables precise delivery of small molecules.
- Antibody-drug conjugates (ADCs) combine antibody specificity with cytotoxic payloads.
Purpose of the Study:
- To describe the bioconjugation process of a vedotin linker-payload onto immunoglobulin G (IgG).
- To detail the subsequent analysis of the generated antibody-drug conjugate (ADC).
- To establish a method for creating targeted therapeutic agents.
Main Methods:
- Utilized bioconjugation techniques to attach a vedotin linker-payload to an IgG.
- Employed analytical methods to characterize the resulting antibody-drug conjugate (ADC).
- Focused on the precise linkage of the payload to the antibody.
Main Results:
- Successfully achieved bioconjugation of the vedotin linker-payload onto IgG.
- Characterized the antibody-drug conjugate (ADC) formed through the described process.
- Demonstrated the feasibility of creating targeted ADCs.
Conclusions:
- The described bioconjugation method is effective for generating antibody-drug conjugates (ADCs).
- This approach facilitates the targeted delivery of small molecule payloads.
- The characterized ADC holds potential for targeted therapeutic applications.
Related Concept Videos
Preparation of Amides
Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
Preparation of 1° Amines: Azide Synthesis
Direct alkylation of ammonia produces polyalkylated amines, along with a quaternary ammonium salt. To exclusively prepare primary amines, the azide synthesis method can be used.
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Preparation of 1° Amines: Gabriel Synthesis
Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
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...
