Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

Prodrugs

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...

Drug Metabolism: Phase II Reactions

Drug Metabolism: Phase II Reactions

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...

Drug Biotransformation: Overview

Drug Biotransformation: Overview

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...

Enzymes

Enzymes

Inside living organisms, enzymes act as catalysts for many biochemical reactions involved in cellular metabolism. The role of enzymes is to reduce the activation energies of biochemical reactions by forming complexes with its substrates. The lowering of activation energies favor an increase in the rates of biochemical reactions.
Enzyme deficiencies can often translate into life-threatening diseases. For example, a genetic abnormality resulting in the deficiency of the enzyme G6PD...

Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

Phase II biotransformation reactions are essential for detoxifying and eliminating xenobiotics, including many pharmaceutical compounds. These reactions typically involve conjugation, the covalent attachment of polar endogenous groups such as glucuronic acid, sulfate, methyl, or acetyl moieties to functional groups introduced during Phase I metabolism. The resulting conjugates are more water-soluble, enabling efficient renal or biliary excretion.The major classes of Phase II enzymes include...

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

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...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Broad-Spectrum Antimicrobial Treatment Targeted Through Drug Conjugation to Vancomycin.

Advanced healthcare materials·2025

Same author

Activation of enzymatic catalysis via nucleic acid hybridization affords synergistic coupling of specificity, potency, and signal amplification.

Nature communications·2025

Same author

Artificial Internalizing Receptors for Targeted Degradation of Extracellular Proteins.

Advanced science (Weinheim, Baden-Wurttemberg, Germany)·2025

Same author

ciRS-7 expression is epigenetically regulated in cancer cells across human adenocarcinomas.

PLoS genetics·2025

Same author

Artificial Biology - Assemble, Imitate, Adapt.

Advanced biology·2025

Same author

Receptor-Mediated Transmembrane Activation of Protein Folding in Synthetic Cells.

Bioconjugate chemistry·2025

Search research articles

Related Experiment Video

Updated: Mar 3, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

Substrate mediated enzyme prodrug therapy.

Betina Fejerskov¹, Morten T Jarlstad Olesen¹, Alexander N Zelikin¹

¹Department of Chemistry and iNano Interdisciplinary Nanoscience Centre, Aarhus University, Denmark.

Advanced Drug Delivery Reviews

|May 2, 2017

Summary

Substrate mediated enzyme prodrug therapy (SMEPT) enables localized drug synthesis using implantable biomaterials. This advanced platform overcomes traditional drug delivery limitations, offering site-specific and flexible therapeutic options.

Keywords:

Controlled delivery Drug delivery Enzyme prodrug therapy

More Related Videos

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

Validation of Therapeutic Agent Conjugation to Polyvinyl Alcohol-Coated Medical Devices

Validation of Therapeutic Agent Conjugation to Polyvinyl Alcohol-Coated Medical Devices

Published on: November 29, 2024

Related Experiment Videos

Last Updated: Mar 3, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

Validation of Therapeutic Agent Conjugation to Polyvinyl Alcohol-Coated Medical Devices

Validation of Therapeutic Agent Conjugation to Polyvinyl Alcohol-Coated Medical Devices

Published on: November 29, 2024

Area of Science:

Biomedical Engineering
Drug Delivery Systems
Biomaterials Science

Background:

Traditional drug administration faces challenges with systemic side effects and variable efficacy.
Implant-mediated drug delivery offers site-specificity but can lack flexibility.
A need exists for localized drug synthesis with enhanced control and versatility.

Purpose of the Study:

To review the historical development and recent advancements in Substrate Mediated Enzyme Prodrug Therapy (SMEPT).
To highlight SMEPT's unique capabilities in localized, site-specific drug synthesis.
To explore future potential and applications of the SMEPT platform.

Main Methods:

Review of historical literature and recent research on SMEPT.
Analysis of SMEPT's mechanism involving implantable biomaterials and enzyme-prodrug interactions.
Evaluation of SMEPT's flexibility in monotherapy, sequential, and combination drug delivery.

Main Results:

SMEPT provides localized drug synthesis via implantable biomaterials.
This platform overcomes drawbacks of oral drugs and traditional implants.
SMEPT allows flexible delivery of multiple drugs and short half-life compounds like nitric oxide.

Conclusions:

SMEPT represents a significant advancement in site-specific drug delivery.
The platform offers unique advantages for localized synthesis and flexible therapeutic strategies.
Further development of SMEPT holds promise for diverse clinical applications.