Drugs acting on DNA topoisomerases: recent advances and future perspectives.

B Gatto, G Capranico, M Palumbo - Current pharmaceutical design, 1999 - europepmc.org
DNA-topoisomerases, a family of DNA-processing enzymes, represent the pharmacological
target of major clinically useful chemotherapeutic agents. These drugs essentially act by …

Mutation of Gly721 alters DNA topoisomerase I active site architecture and sensitivity to camptothecin

M Van Der Merwe, MA Bjornsti - Journal of biological chemistry, 2008 - ASBMB
DNA topoisomerase I (Top1p) catalyzes the relaxation of supercoiled DNA via a concerted
mechanism of DNA strand cleavage and religation. Top1p is the cellular target of the anti …

Change of the sequence specificity of daunorubicin-stimulated topoisomerase II DNA cleavage by epimerization of the amino group of the sugar moiety

G Capranico, E Butelli, F Zunino - Cancer research, 1995 - AACR
Antitumor drugs stimulate topoisomerase II-mediated DNA cleavage in a DNA sequence-
specific manner. The drug sequence specificity is often very similar among antitumor agents …

The mechanism of topoisomerase I poisoning by a camptothecin analog

BL Staker, K Hjerrild, MD Feese… - Proceedings of the …, 2002 - National Acad Sciences
We report the x-ray crystal structure of human topoisomerase I covalently joined to double-
stranded DNA and bound to the clinically approved anticancer agent Topotecan. Topotecan …

Specific interaction of camptothecin, a topoisomerase I inhibitor, with guanine residues of DNA detected by photoactivation at 365 nm

F Leteurtre, M Fesen, G Kohlhagen, KW Kohn… - Biochemistry, 1993 - ACS Publications
Revised Manuscript Received June 8, 1993 abstract: Camptothecin-induced DNA
photolesions were examined after UVA irradiation at 365 nm. DNA single-strand breaks …

DNA topoisomerase I-mediated formation of structurally modified DNA duplexes. Effects of metal ions and topoisomerase I inhibitors

X Wang, KA Henningfeld, SM Hecht - Biochemistry, 1998 - ACS Publications
The ability of DNA topoisomerase I to mediate the formation of structurally modified DNA
duplexes was studied utilizing suicide substrates containing high-efficiency cleavage sites …

Role of flexibility in protein‐DNA‐drug recognition: The case of Asp677Gly‐Val703Ile topoisomerase mutant hypersensitive to camptothecin

ID′ Annessa, C Tesauro, P Fiorani… - Journal of amino …, 2012 - Wiley Online Library
Topoisomerases I are ubiquitous enzymes that control DNA topology within the cell. They
are the unique target of the antitumor drug camptothecin that selectively recognizes the DNA …

Dual role of glutathione in modulating camptothecin activity: depletion potentiates activity, but conjugation enhances the stability of the topoisomerase I-DNA cleavage …

MP Gamcsik, MS Kasibhatla, DJ Adams… - Molecular Cancer …, 2001 - AACR
Depletion of glutathione (GSH) in MCF-7 and MDA-MB-231 cell lines by pretreatment with
the GSH synthesis inhibitor buthionine sulfoximine potentiated the activity of 10, 11 …

Camptothecin-stabilised topoisomerase I–DNA complexes in leukaemia cells visualised and quantified in Situ by the TARDIS Assay (trapped in agarose DNA …

K Padget, R Carr, ADJ Pearson, MJ Tilby… - Biochemical …, 2000 - Elsevier
We have shown that the TARDIS assay (t rapped in a gar ose D NA i mmunos taining) can
be used to detect DNA–topoisomerase I (topo I) cleavable complexes in situ in individual …

Mode of action of topoisomerase II-targeting agents at a specific DNA sequence: uncoupling the DNA binding, cleavage and religation events

BS Sørensen, J Sinding, AH Andersen, J Alsner… - Journal of molecular …, 1992 - Elsevier
Methods for uncoupling the DNA binding, cleavage and religation reactions of
topoisomerase II were employed to investigate the influence of topoisomerase II-directed …