Related Experiment Video
Updated: Jul 29, 2025
09:14
Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
Published on: July 20, 2016
39.0K
Enzymatic Bioconjugation: A Perspective from the Pharmaceutical Industry
Aaron Debon1, Elina Siirola1, Radka Snajdrova1
1Global Discovery Chemistry, Novartis Institute for Biomedical Research, Basel 4108, Switzerland.
JACS Au
|May 26, 2023
Summary
Enzymes offer precise bioconjugation for macromolecules, advancing drug development. This perspective explores enzymatic methods, highlighting successes and future opportunities in bioconjugation chemistry.
Area of Science:
- Biochemistry and Chemical Biology
- Drug Discovery and Development
Background:
- Enzymes are highly selective catalysts for small molecule synthesis in pharmaceuticals.
- Enzymatic catalysis offers potential for macromolecule modification and bioconjugate formation.
- Existing bioorthogonal chemistries present significant competition for enzymatic methods.
Purpose of the Study:
- To illuminate the applications of enzymatic bioconjugation for novel drug modalities.
- To highlight current successes and challenges of enzymatic bioconjugation in drug development pipelines.
- To identify opportunities for advancing enzymatic bioconjugation technologies.
Main Methods:
- Review and analysis of current literature on enzymatic bioconjugation.
- Case studies of enzymatic applications in pharmaceutical research and development.
- Comparative assessment of enzymatic versus non-enzymatic bioconjugation strategies.
Main Results:
- Enzymes demonstrate exquisite selectivity and rate acceleration for bioconjugation.
- Successful examples of enzymatic bioconjugation in various stages of drug development were identified.
- Specific pitfalls and limitations of current enzymatic approaches were discussed.
Conclusions:
- Enzymatic bioconjugation holds significant promise for creating advanced bioconjugates.
- Further development is needed to overcome existing challenges and expand enzyme applications.
- Enzymatic methods offer a valuable complementary approach to existing bioorthogonal chemistries in drug development.
More Related Videos
Related Concept Videos
01:14Phase II Conjugation Reactions: Overview
254
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...
254
01:16Drug Biotransformation: Overview
2.5K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
2.5K
01:14Drug Metabolism: Phase II Reactions
3.9K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
3.9K
01:19Phase II Reactions: Sulfation and Conjugation with α-Amino Acids
304
Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
304