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Review

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

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College of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave, Purdue University, West Lafayette, IN 47907, USA
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Center for Cancer Research, Purdue University, 201 S University St, West Lafayette, IN 47906, USA
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Department of Chemistry, Purdue University, West Lafayette, IN 47906, USA
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Purdue Institute for Drug Discovery, West Lafayette, IN 47906, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Molecules 2021, 26(14), 4132; https://doi.org/10.3390/molecules26144132
Received: 28 April 2021 / Revised: 18 June 2021 / Accepted: 29 June 2021 / Published: 7 July 2021
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. View Full-Text
Keywords: XR5944; MLN944; anticancer drug; DNA; NMR; bis-intercalator; major groove binder XR5944; MLN944; anticancer drug; DNA; NMR; bis-intercalator; major groove binder
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MDPI and ACS Style

Buric, A.J.; Dickerhoff, J.; Yang, D. Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action. Molecules 2021, 26, 4132. https://doi.org/10.3390/molecules26144132

AMA Style

Buric AJ, Dickerhoff J, Yang D. Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action. Molecules. 2021; 26(14):4132. https://doi.org/10.3390/molecules26144132

Chicago/Turabian Style

Buric, Adam J., Jonathan Dickerhoff, and Danzhou Yang. 2021. "Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action" Molecules 26, no. 14: 4132. https://doi.org/10.3390/molecules26144132

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