Results 231 to 240 of about 61,437 (248)
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Topoisomerase I Inhibitors – The Camptothecins

2010
The camptothecins are a class of antineoplastic agents that inhibit the enzyme DNA topoisomerase I and have established activity in the treatment of various human malignancies. Camptothecin (CPT) was originally isolated in 1966 from the bark and stem of the native Chinese tree, Campotheca acuminate [155].
Michael Newton   +2 more
openaire   +1 more source

Review : Topoisomerase I inhibitors: 2. Irinotecan

Journal of Oncology Pharmacy Practice, 1998
Purpose. The primary objective of this article is to discuss the pharmacology, pharmacokinetics, clinical use, and adverse effects of the approved topoisomer ase I inhibitors. This is the second in a series of two articles and will focus on irinotecan. Data Sources.
J. Andrew Skirvin, Valerie Relias
openaire   +1 more source

Review : Topoisomerase I inhibitors: 1. Topotecan

Journal of Oncology Pharmacy Practice, 1997
Purpose. The primary objective of this article is to discuss the pharmacology, pharmacokinetics, clin ical use, and adverse effects of the approved topoisomerase I inhibitors. This is the first in a series of two articles and will focus on topotecan. Data Sources.
Valerie Relias, J. Andrew Skirvin
openaire   +1 more source

Quadruplex-Duplex Motifs as New Topoisomerase I Inhibitors

Nucleosides, Nucleotides & Nucleic Acids, 2010
In this article, 13 short chains that can form G-quadruplex and quadruplex-duplex motif have been designed. Fourteen oligonucleotides, including 13 short chains as well as a reference short chain all have certain level of inhibition to topoisomerase I, whether or not they form G-quadruplex and quadruplex-duplex motif, and the G-quadruplex and ...
Li, Shuai   +4 more
openaire   +2 more sources

Inhibitors of Topoisomerase I Function

2005
As noted elsewhere in this book, the locus of action of camptothecin (CPT) (1) (Fig. 1) as an antitumor agent involves the noncovalent binding of this agent to the covalent binary complex formed between topoisomerase I (TOP-I) and DNA (Fig. 2) (1). Although the equilibrium between free enzyme and the enzyme-DNA binary complex normally lies far toward ...
openaire   +1 more source

Diversity of DNA topoisomerases I and inhibitors

Biochimie, 1998
The present review first describes the different type I topoisomerases found in eukaryotic cells: nuclear topoisomerase I (top1), topoisomerase 3 (top3), mitochondrial topoisomerase I and viral topoisomerases I. The second part of the review provides extensive information on the topoisomerase I inhibitors identified to date.
openaire   +2 more sources

Dual Topoisomerase I / II Inhibitors in Cancer Therapy

Current Topics in Medicinal Chemistry, 2003
While the majority of topoisomerase (topo) inhibitors show selectivity against either topo I or topo II, a small class of compounds can act against both enzymes. These can be divided into three classes. The first and largest class comprise drugs that bind to DNA by intercalation and include the clinically-evaluated acridine DACA, the benzopyridoindole ...
William A, Denny, Bruce C, Baguley
openaire   +2 more sources

Nick-containing oligonucleotides as human topoisomerase I inhibitors

Bioorganic & Medicinal Chemistry Letters, 2009
A series of oligonucleotides with various lengths that contain nick and topoisomerase I-binding sites were designed. The interactions between these oligonucleotides and human topoisomerase I were investigated and the most efficient one among them has displayed IC(50) value of 6.3 nM.
Sock Teng, Chua   +9 more
openaire   +2 more sources

Topoisomerase I Inhibitors: Chemical Biology

2011
Topoisomerase I (Top1), an essential enzyme, produces a DNA single-strand break allowing DNA relaxation for replication. The enzymatic mechanism involves sequential transesterifications and the reaction is freely reversible. The Top1 reaction intermediate consists of enzyme covalently linked to DNA, thus a “cleavable complex”. Covalently bound Top1-DNA
openaire   +1 more source

Clinical pharmacokinetics of camptothecin topoisomerase I inhibitors.

Pharmacy world & science : PWS, 1998
In this review the clinical pharmacokinetics of camptothecin topoisomerase I inhibitors, an important new class of anticancer drugs, is discussed. Two prototypes, topotecan and irinotecan, are currently marketed in many European countries and the USA for the treatment of patients with ovarian and colorectal cancer, respectively.
Herben, V.M.M.   +3 more
openaire   +2 more sources

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