Related Experiment Video
Updated: Jun 12, 2026

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Targeted enzyme prodrug therapies
N Schellmann1, P M Deckert, D Bachran
1Zentralinstitut für Laboratoriumsmedizin und Pathobiochemie, Charité - Universitätsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 30, D-12200 Berlin, Germany.
Targeted cancer therapies, including enzyme prodrug strategies, offer new hope for difficult-to-treat tumors. These innovative treatments aim to specifically activate drugs at the tumor site, improving efficacy and reducing side effects.
Area of Science:
- Oncology
- Biochemistry
- Pharmacology
Background:
- Cancer treatment faces challenges with invasive, metastatic, and inaccessible tumors despite traditional methods like surgery, chemotherapy, and radiotherapy.
- Targeted therapies have emerged over the last three decades to specifically locate, detect, and eliminate tumor cells.
- Tumor site-specific prodrug activation is a promising two-step targeted therapy approach.
Purpose of the Study:
- To provide a concise overview of the history and latest developments in targeted cancer therapies.
- To review key technologies in targeted cancer treatment, focusing on enzyme prodrug strategies.
- To highlight advancements in prodrug-converting enzymes, prodrugs, and drugs for cancer therapy.
Main Methods:
- Review of historical and recent scientific literature on targeted cancer therapies.
- Analysis of enzyme prodrug therapy concepts and their evolution since 1974.
- Examination of various targeting systems including antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), clostridial- (CDEPT), and polymer-directed enzyme prodrug therapy (PDEPT).
Main Results:
- Significant progress has been made in developing targeted therapies, particularly those involving enzyme-mediated prodrug activation.
- Various targeting systems, enzymes, and prodrugs have been investigated and refined over the years.
- The review covers a range of enzyme prodrug therapy approaches and their components.
Conclusions:
- Enzyme prodrug therapy represents a significant advancement in the quest for more effective and specific cancer treatments.
- Continued research and development in targeting systems, enzymes, and prodrugs are crucial for overcoming challenges in cancer cure.
- Targeted therapies, especially ADEPT and GDEPT, offer a promising alternative for treating difficult cancers.
Related Concept Videos
Prodrugs
Prodrugs help overcome...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Modified-Release Drug Delivery Systems: Site-Targeted
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Pharmacogenomics: Identification of New Drug Targets

