Small molecule microarray identifies inhibitors of tyrosyl-DNA phosphodiesterase 1 that simultaneously access the catalytic pocket and two substrate binding sites-Reference-Cited by-同舟云学术

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Small molecule microarray identifies inhibitors of tyrosyl-DNA phosphodiesterase 1 that simultaneously access the catalytic pocket and two substrate binding sites

Published:2021 Issue:11 Volume:12 Page:3876-3884
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Zhao Xue Zhi¹²³⁴⁵^ORCID,Kiselev Evgeny⁶⁷²³⁸,Lountos George T.⁹¹⁰⁴⁵^ORCID,Wang Wenjie⁶⁷²³⁸,Tropea Joseph E.¹¹²³⁴⁵,Needle Danielle¹¹²³⁴⁵,Hilimire Thomas A.¹²³⁴⁵,Schneekloth John S.¹²³⁴⁵^ORCID,Waugh David S.¹¹²³⁴⁵,Pommier Yves⁶⁷²³⁸,Burke Terrence R.¹²³⁴⁵^ORCID

Affiliation:

1. Chemical Biology Laboratory

2. Center for Cancer Research

3. National Cancer Institute

4. Frederick

5. USA

6. Developmental Therapeutics Branch

7. Laboratory of Molecular Pharmacology

8. Bethesda

9. Basic Science Program

10. Frederick National Laboratory for Cancer Research

11. Center for Structural Biology

Abstract

Using small molecule microarray TDP1 inhibitors have been identified that bind in a trivalent mode.

Funder

National Cancer Institute

Frederick National Laboratory for Cancer Research

National Institutes of Health

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/SC/D0SC05411A

Reference42 articles.

1. Tyrosyl–DNA phosphodiesterases: rescuing the genome from the risks of relaxation

2. TDP1 Overexpression in Human Cells Counteracts DNA Damage Mediated by Topoisomerases I and II

3. DNA Topoisomerase I Inhibitors: Chemistry, Biology, and Interfacial Inhibition

4. Tyrosyl-DNA Phosphodiesterase 1 Targeting for Modulation of Camptothecin-Based Treatment

5. Tyrosyl-DNA-phosphodiesterases (TDP1 and TDP2)

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4. New Dual Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 and 2 Based on Deoxycholic Acid: Design, Synthesis, Cytotoxicity, and Molecular Modeling;Molecules;2024-01-24

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