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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| Format: | Article |
| Language: | English |
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MDPI AG
2021-07-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/14/4132 |
| _version_ | 1827687295185059840 |
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| author | Adam J. Buric Jonathan Dickerhoff Danzhou Yang |
| author_facet | Adam J. Buric Jonathan Dickerhoff Danzhou Yang |
| author_sort | Adam J. Buric |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-03-10T09:31:32Z |
| format | Article |
| id | doaj.art-70d807c57be24335a4d92fdf981591e7 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T09:31:32Z |
| publishDate | 2021-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-70d807c57be24335a4d92fdf981591e72023-11-22T04:29:02ZengMDPI AGMolecules1420-30492021-07-012614413210.3390/molecules26144132Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of ActionAdam J. Buric0Jonathan Dickerhoff1Danzhou Yang2College of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave, Purdue University, West Lafayette, IN 47907, USACollege of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave, Purdue University, West Lafayette, IN 47907, USACollege of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave, Purdue University, West Lafayette, IN 47907, USAThis 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.https://www.mdpi.com/1420-3049/26/14/4132XR5944MLN944anticancer drugDNANMRbis-intercalator |
| spellingShingle | Adam J. Buric Jonathan Dickerhoff Danzhou Yang Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action Molecules XR5944 MLN944 anticancer drug DNA NMR bis-intercalator |
| 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 | XR5944 MLN944 anticancer drug DNA NMR bis-intercalator |
| url | https://www.mdpi.com/1420-3049/26/14/4132 |
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