Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action

This review is dedicated to Professor William A. Denny’s discovery of XR5944 (also known as MLN944). XR5944 is a DNA-targeted agent with exceptionally potent antitumor activity and a novel DNA binding mode, bis-intercalation and major groove binding, as well as a novel mechanism of action, transcrip...

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Detalles Bibliográficos
Autores principales: Buric, Adam J., Dickerhoff, Jonathan, Yang, Danzhou
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8304338/
https://www.ncbi.nlm.nih.gov/pubmed/34299405
http://dx.doi.org/10.3390/molecules26144132
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author Buric, Adam J.
Dickerhoff, Jonathan
Yang, Danzhou
author_facet Buric, Adam J.
Dickerhoff, Jonathan
Yang, Danzhou
author_sort Buric, Adam J.
collection PubMed
description This review is dedicated to Professor William A. Denny’s discovery of XR5944 (also known as MLN944). XR5944 is a DNA-targeted agent with exceptionally potent antitumor activity and a novel DNA binding mode, bis-intercalation and major groove binding, as well as a novel mechanism of action, transcription inhibition. This novel anticancer compound represents a remarkable accomplishment resulting from two decades of drug discovery by Professor Denny and coworkers. Here, we review our work on the structural study of the DNA binding mode of XR5944 and mechanistic study of XR5944 action.
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spelling pubmed-83043382021-07-25 Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action Buric, Adam J. Dickerhoff, Jonathan Yang, Danzhou Molecules Review This review is dedicated to Professor William A. Denny’s discovery of XR5944 (also known as MLN944). XR5944 is a DNA-targeted agent with exceptionally potent antitumor activity and a novel DNA binding mode, bis-intercalation and major groove binding, as well as a novel mechanism of action, transcription inhibition. This novel anticancer compound represents a remarkable accomplishment resulting from two decades of drug discovery by Professor Denny and coworkers. Here, we review our work on the structural study of the DNA binding mode of XR5944 and mechanistic study of XR5944 action. MDPI 2021-07-07 /pmc/articles/PMC8304338/ /pubmed/34299405 http://dx.doi.org/10.3390/molecules26144132 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Buric, Adam J.
Dickerhoff, Jonathan
Yang, Danzhou
Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title_full Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title_fullStr Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title_full_unstemmed Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title_short Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action
title_sort novel dna bis-intercalator xr5944 as a potent anticancer drug—design and mechanism of action
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8304338/
https://www.ncbi.nlm.nih.gov/pubmed/34299405
http://dx.doi.org/10.3390/molecules26144132
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