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

XZ Zhao, E Kiselev, GT Lountos, W Wang… - Chemical …, 2021 - pubs.rsc.org
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a member of the phospholipase D family of
enzymes, which catalyzes the removal of both 3′-and 5′-DNA phosphodiester adducts …

Identification of a ligand binding hot spot and structural motifs replicating aspects of tyrosyl-DNA phosphodiesterase I (TDP1) phosphoryl recognition by …

GT Lountos, XZ Zhao, E Kiselev, JE Tropea… - Nucleic Acids …, 2019 - academic.oup.com
Abstract Tyrosyl DNA-phosphodiesterase I (TDP1) repairs type IB topoisomerase (TOP1)
cleavage complexes generated by TOP1 inhibitors commonly used as anticancer agents …

Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime …

XZ Zhao, W Wang, GT Lountos, E Kiselev… - RSC Chemical …, 2023 - pubs.rsc.org
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a member of the phospholipase D family that
can downregulate the anticancer effects of the type I topoisomerase (TOP1) inhibitors by …

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay

C Marchand, WA Lea, A Jadhav, TS Dexheimer… - Molecular cancer …, 2009 - AACR
Abstract Tyrosyl-DNA phosphodiesterase I (Tdp1) resolves topoisomerase I (Top1)-DNA
adducts accumulated from natural DNA damage as well as from the action of certain …

Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft

BR Kossmann, M Abdelmalak, S Lopez… - Bioorganic & medicinal …, 2016 - Elsevier
Abstract Tyrosyl-DNA phosphodiesterase 2 (TDP2) processes protein/DNA adducts
resulting from abortive DNA topoisomerase II (Top2) activity. TDP2 inhibition could provide …

New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2)

CJA Ribeiro, J Kankanala, K Shi, K Kurahashi… - European Journal of …, 2018 - Elsevier
Abstract Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2)
mediated DNA damages and causes resistance to TOP2-targeted cancer therapy. Inhibiting …

5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl–DNA phosphodiesterase I

VR Sirivolu, SKV Vernekar, C Marchand… - Journal of medicinal …, 2012 - ACS Publications
Tyrosyl–DNA phosphodiesterase I (Tdp1) is a cellular enzyme that repairs the irreversible
topoisomerase I (Top1)–DNA complexes and confers chemotherapeutic resistance to Top1 …

A fluorescence-based assay for the apurinic/apyrimidinic-site cleavage activity of human tyrosyl-DNA phosphodiesterase 1

GJ Thomson, NS Hamilton, GV Hopkins… - Analytical …, 2013 - Elsevier
Abstract Tyrosyl-DNA phosphodiesterase 1 (Tdp1) catalyzes the hydrolysis of
phosphodiester bonds between the DNA 3′-phosphate and tyrosine residues and plays a …

Promising new inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 4-arylcoumarin and monoterpenoid moieties as components of complex antitumor …

TM Khomenko, AL Zakharenko, AA Chepanova… - International Journal of …, 2019 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an important DNA repair enzyme in humans,
and a current and promising inhibition target for the development of new chemosensitizing …

Isoquinoline-1, 3-diones as selective inhibitors of tyrosyl DNA phosphodiesterase II (TDP2)

J Kankanala, C Marchand, M Abdelmalak… - Journal of medicinal …, 2016 - ACS Publications
Tyrosyl DNA phosphodiesterase II (TDP2) is a recently discovered enzyme that specifically
repairs DNA damages induced by topoisomerase II (Top2) poisons and causes resistance to …