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DNA Topoisomerases

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. ...

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Related Experiment Video

Updated: Jan 16, 2026

Simple and Fast Rolling Circle Amplification-Based Detection of Topoisomerase 1 Activity in Crude Biological Samples

Simple and Fast Rolling Circle Amplification-Based Detection of Topoisomerase 1 Activity in Crude Biological Samples

Published on: December 2, 2022

In silico Study of Novel Tryptanthrin-Based Topoisomerase Inhibitors.

Mukesh Kumar Kumawat¹, Kapil Kumar²

¹School of Pharmaceutical Sciences, Apeejay Stya University, Gurugram, Haryana, 122103, India.

Medicinal Chemistry (Shariqah (United Arab Emirates))

|September 26, 2025

Summary

Researchers designed novel tryptanthrin analog hybrids for cancer drug discovery. Six potent compounds showed superior DNA topoisomerase inhibition compared to existing drugs in silico, paving the way for new anticancer therapies.

Keywords:

ATPase domain Tryptanthrin antitumor.glide extra precision docking molinspiration pharmacokinetics topoisomerase IIα

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Last Updated: Jan 16, 2026

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Area of Science:

Medicinal Chemistry
Computational Drug Design
Pharmacology

Background:

Cancer drug research has evolved significantly, with traditional therapies targeting DNA, DNA production, cell division, or microtubules.
Tryptanthrin and its analogs show promise for anticancer applications.

Purpose of the Study:

To design novel tryptanthrin analogs with potential anticancer activity.
To identify potent DNA topoisomerase inhibitors through computational methods.

Main Methods:

Synthesized 72 tryptanthrin derivatives by modifying the C-6 carbonyl position.
Performed in silico molecular docking against DNA topoisomerase using doxorubicin and teniposide as references.
Conducted in silico ADMET studies to assess drug-likeness.

Main Results:

Six selected ligands (RC 51, RC 29, RC 42, RC 3, RC 54, RC 63) exhibited stronger binding affinity than reference drugs.
These compounds demonstrated potential as DNA topoisomerase inhibitors.

Conclusions:

The computational approach successfully identified potent topoisomerase inhibitors.
The identified ligands warrant further in vitro and in vivo investigation for anticancer efficacy.