Topoisomerase I inhibitors: Challenges, progress and the road ahead

A Talukdar, B Kundu, D Sarkar, S Goon… - European Journal of …, 2022 - Elsevier
Abstract Topoisomerase IB (Top1), a subcategory of DNA topoisomerase enzymes is
expressed much higher in several tumor cells. Therefore, modulating the activity of Top1 in …

[HTML][HTML] Copper complexes as anticancer agents targeting topoisomerases I and II

C Molinaro, A Martoriati, L Pelinski, K Cailliau - Cancers, 2020 - mdpi.com
Simple Summary Organometallics, such as copper compounds, are cancer
chemotherapeutics used alone or in combination with other drugs. One small group of …

[HTML][HTML] Natural products and their derivatives as inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1

AL Zakharenko, OA Luzina, AA Chepanova… - International Journal of …, 2023 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an important repair enzyme that removes
various covalent adducts from the 3′ end of DNA. Particularly, covalent complexes of …

The design and discovery of topoisomerase I inhibitors as anticancer therapies

E Martín-Encinas, A Selas, F Palacios… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Cancer has been identified as one of the leading causes of death worldwide.
The biological target of some anticancer agents is topoisomerase I, an enzyme involved in …

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

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 …

[HTML][HTML] The role of single strand break repair pathways in cellular responses to camptothecin induced DNA damage

C Mei, L Lei, LM Tan, XJ Xu, BM He, C Luo… - Biomedicine & …, 2020 - Elsevier
Efficient DNA repair is critical for cell survival following exposure to DNA topoisomerase I
(Top1) inhibitors camptothecin, a nature product from which the common chemotherapeutic …

The influence of an enamine usnic acid derivative (a tyrosyl-DNA phosphodiesterase 1 inhibitor) on the therapeutic effect of topotecan against transplanted tumors in …

VP Nikolin, NA Popova, VI Kaledin, OA Luzina… - Clinical & Experimental …, 2021 - Springer
Abstract Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a repair enzyme for 3′-end DNA
lesions, predominantly stalled DNA–topoisomerase 1 (Top1) cleavage complexes. Tdp1 is a …

[HTML][HTML] New hybrid compounds combining fragments of usnic acid and thioether are inhibitors of human enzymes TDP1, TDP2 and PARP1

NS Dyrkheeva, AS Filimonov, OA Luzina… - International Journal of …, 2021 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (TDP1) catalyzes the cleavage of the phosphodiester
bond between the tyrosine residue of topoisomerase 1 (TOP1) and the 3′ phosphate of …

[HTML][HTML] Design, synthesis, and biological investigation of novel classes of 3-carene-derived potent inhibitors of TDP1

IV Il'ina, NS Dyrkheeva, AL Zakharenko, AY Sidorenko… - Molecules, 2020 - mdpi.com
Two novel structural types of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors with
hexahydroisobenzofuran 11 and 3-oxabicyclo [3.3. 1] nonane 12 scaffolds were discovered …

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

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 …