Fluorogenic probes for disease-relevant enzymes

J Zhang, X Chai, XP He, HJ Kim, J Yoon… - Chemical Society …, 2019 - pubs.rsc.org
Traditional biochemical methods for enzyme detection are mainly based on antibody-based
immunoassays, which lack the ability to monitor the spatiotemporal distribution and, in …

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 …

Monoallelic variation in DHX9, the gene encoding the DExH-box helicase DHX9, underlies neurodevelopment disorders and Charcot-Marie-Tooth disease

DG Calame, T Guo, C Wang, L Garrett, A Jolly… - The American Journal of …, 2023 - cell.com
DExD/H-box RNA helicases (DDX/DHX) are encoded by a large paralogous gene family; in
a subset of these human helicase genes, pathogenic variation causes neurodevelopmental …

Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study

C Tesauro, AK Simonsen, MB Andersen, KW Petersen… - BMC cancer, 2019 - Springer
Background Camptothecin (CPT) and its derivatives are currently used as second-or third-
line treatment for patients with endocrine-resistant breast cancer (BC). These drugs convert …

New inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 7-hydroxycoumarin and monoterpenoid moieties

T Khomenko, A Zakharenko, T Odarchenko… - Bioorganic & Medicinal …, 2016 - Elsevier
A number of derivatives of 7-hydroxycoumarins containing aromatic or monoterpene
substituents at hydroxy-group were synthesized based on a hit compound from a virtual …

[HTML][HTML] Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan

AA Munkuev, NS Dyrkheeva, TE Kornienko, ES Ilina… - Molecules, 2022 - mdpi.com
Inhibiting tyrosyl-DNA phosphodiesterase 1 (TDP1) is a promising strategy for increasing the
effectiveness of existing antitumor therapy since it can remove the DNA lesions caused by …

A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold

NS Li-Zhulanov, AL Zakharenko, AA Chepanova… - Molecules, 2018 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that mends
topoisomerase 1-mediated DNA damage. Tdp1 is a current inhibition target for the …

Aminoadamantanes containing monoterpene-derived fragments as potent tyrosyl-DNA phosphodiesterase 1 inhibitors

KY Ponomarev, EV Suslov, AL Zakharenko… - Bioorganic …, 2018 - Elsevier
The ability of a number of nitrogen-containing compounds that simultaneously carry the
adamantane and monoterpene moieties to inhibit Tdp1, an important enzyme of the DNA …

[HTML][HTML] The development of Tyrosyl-DNA phosphodiesterase 1 inhibitors. Combination of monoterpene and adamantine moieties via amide or thioamide bridges

AA Chepanova, ES Mozhaitsev, AA Munkuev… - Applied Sciences, 2019 - mdpi.com
Featured Application Inhibition of Tdp1 has the potential to increase the potency of the
anticancer drugs topotecan and irinotecan, topoisomerase 1 poisons. Furthermore, Tdp1 …

TDP1 and PARP1 deficiency are cytotoxic to rhabdomyosarcoma cells

HK Fam, C Walton, SA Mitra, M Chowdhury… - Molecular Cancer …, 2013 - aacrjournals.org
Rhabdomyosarcoma is the most common soft tissue sarcoma in children. Metastatic
rhabdomyosarcoma in children has a 5-year event-free survival rate of< 30%, and a recent …