Related Experiment Video

Updated: Jan 27, 2026

Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
08:03

Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles

Published on: December 1, 2016

9.5K

Topoisomerase Inhibitors and Targeted Delivery in Cancer Therapy

Fei You1, Changshou Gao1

  • 1Antibody Discovery and Protein Engineering, MedImmune, One MedImmune Way, Gaithersburg, MD 20878, United States.

Current Topics in Medicinal Chemistry
|April 2, 2019
PubMed

Insights

DNA topoisomerases are crucial enzymes for DNA replication and are key cancer chemotherapy targets. New inhibitors aim to improve efficacy and reduce side effects through targeted delivery strategies.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Cancer Therapeutics

Background:

  • DNA topoisomerases regulate DNA topology, essential for cellular processes like replication.
  • Topoisomerases are validated targets in cancer chemotherapy, with existing drugs offering significant efficacy but notable side effects.
  • Developing next-generation topoisomerase inhibitors and targeted delivery systems is a major focus in oncology.

Purpose of the Study:

  • To explore the role of DNA topoisomerases as cancer targets.
  • To review current and emerging strategies for topoisomerase inhibitor development.
  • To highlight the potential of targeted delivery to mitigate side effects of topoisomerase inhibitors.

Main Methods:

  • Review of existing literature on DNA topoisomerases and their inhibitors.
  • Analysis of clinical applications and limitations of current topoisomerase-targeting drugs.
  • Examination of novel strategies for targeted delivery of anticancer agents.

Main Results:

  • Topoisomerase I and II inhibitors are clinically effective anticancer agents.
  • Significant side effects are associated with current topoisomerase inhibitors.
  • Targeted delivery approaches, including antibody and polymer conjugates, show promise for reducing toxicity.

Conclusions:

  • DNA topoisomerases remain critical targets for cancer treatment.
  • Advancements in inhibitor design and targeted delivery are essential for improving therapeutic outcomes.
  • Targeted strategies offer a viable path to enhance the safety and efficacy of topoisomerase-based cancer therapies.
Keywords:
Cancer targetDNA strain breakTargeted deliveryTopoisomeraseTopoisomerase inhibitorsTopology of DNA.

More Related Videos

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors08:45

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors

Published on: July 17, 2020

6.6K
Proton Therapy Delivery and Its Clinical Application in Select Solid Tumor Malignancies08:34

Proton Therapy Delivery and Its Clinical Application in Select Solid Tumor Malignancies

Published on: February 6, 2019

21.0K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
8.7K
DNA Topoisomerases02:02

DNA Topoisomerases

Topoisomerases are enzymes that relax overwound DNA molecules during various cell processes, including DNA replication and transcription. These enzymes regulate positive and negative DNA supercoiling without changing the nucleotide sequence. DNA overwinding in a clockwise direction results in positively supercoiled DNA, whereas underwinding in a counterclockwise direction produces negatively supercoiled DNA.
Types and Mechanism of action
Topoisomerases are divided into two main types. ...
35.3K
Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
9.9K
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
10.9K
Gene Therapy00:59

Gene Therapy

Gene therapy is a technique where a gene is inserted into a person’s cells to prevent or treat a serious disease. The added gene may be a healthy version of the gene that is mutated in the patient, or it could be a different gene that inactivates or compensates for the patient’s disease-causing gene. For example, in patients with severe combined immunodeficiency (SCID) due to a mutation in the gene for the enzyme adenosine deaminase, a functioning version of the gene can be...
27.4K
Group Therapy01:26

Group Therapy

Group therapy is a sociocultural approach to psychological treatment, where individuals with shared psychological challenges come together under the guidance of a mental health professional. This therapeutic modality offers unique opportunities for individuals to connect, share, and grow within the context of a supportive group. By fostering mutual understanding and collaboration, group therapy can address a range of psychological concerns effectively, often complementing or surpassing the...
410