Open AccessJournal Article
Identification of Topoisomerase I as the Cytotoxic Target of the Protoberberine Alkaloid Coralyne
Barbara Gatto,Marilyn M. Sanders,Chiang Yu,Hong Yan Wu,Makhey Darshan B,Edmond J. LaVoie,Leroy-Fong Liu +6 more
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TLDR
It seems possible to develop coralyne and nitidine derivatives as new topo I-targeted therapeutics to overcome aspects of camptothecin-related resistance.Abstract:
Protoberberine alkaloids (coralyne and its derivatives), which exhibit antileukemic activity in animal models, have been shown to be potent inducers of topoisomerase (topo) I-DNA cleavable complexes using purified recombinant human DNA topo I Different from the structurally similar benzophenanthridine alkaloid nitidine (a dual poison of both topos I and II), coralyne and its derivatives have marginal poisoning activity against DNA topo II Yeast cells expressing human DNA topo I are shown to be specifically sensitive to killing by coralyne derivatives and nitidine, suggesting that cellular DNA topo I is their cytotoxic target Two human camptothecin-resistant cell lines, CPT-K5 and A2780/CPT-2000, which are known to express highly camptothecin-resistant topo I, are only marginally resistant to coralyne derivatives and nitidine Purification of human topo I from Escherichia coli cells overexpressing CPT-K5 recombinant topo I has demonstrated similar marginal cross-resistance to nitidine It seems possible to develop coralyne and nitidine derivatives as new topo I-targeted therapeutics to overcome aspects of camptothecin-related resistanceread more
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Patent
Fluorescent silica-based nanoparticles
Ulrich Wiesner,Hooisweng Ow +1 more
TL;DR: In this paper, a core comprising a fluorescent silane compound; and a silica shell on the core is presented. And methods for the preparation of nanoparticle compositions including fluorescent nanoparticles, ligated-fluorescent nanoparticles having therapeutic agents, and coupled or associated with an analyte are presented.
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Mechanism of action of eukaryotic dna topoisomerase i and drugs targeted to the enzyme
TL;DR: The present review describes the topoisomerase I catalytic mechanisms with particular emphasis on the cleavage complex that represents the enzyme's catalytic intermediate and the site of action for camptothecins.
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Berberine: new perspectives for old remedies.
TL;DR: A growing body of reports supports the evidence that berberine has anticancer effects, being able to block the proliferation of and to kill cancer cells.
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Topoisomerase I inhibitors: Review and update
TL;DR: The challenge for the next five years is to identify ways to integrate the topo I inhibitors into multidrug and multimodality therapies to achieve optimal antitumour effect, while keeping the side effects of these therapies manageable.
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Therapeutic potential of nucleic acid-binding isoquinoline alkaloids: binding aspects and implications for drug design.
TL;DR: Up‐to‐date details of the interaction of berberine, palmatine, and jatrorrhizine of the protoberberine group, sanguinarine from the benzophananthridines group, and several of their synthetic derivatives, such as coralyne, berberrubine,Palmatrubin, andJatrorubin with nucleic acids have been reviewed.
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Journal ArticleDOI
Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays
TL;DR: A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.
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Rapid colorimetric assay for cell growth and survival. Modifications to the tetrazolium dye procedure giving improved sensitivity and reliability.
François Denizot,Rita Lang +1 more
TL;DR: The reliability and sensitivity of the test have been increased to the point where it can in many cases replace the [3H]thymidine uptake assay to measure cell proliferation or survival in growth factor or cytotoxicity assays.
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Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I.
TL;DR: It is proposed that camptothecin blocks the rejoining step of the breakage-reunion reaction of mammalian DNA topoisomerase I, which results in the accumulation of a cleavable complex which resembles the transient intermediate proposed for eukaryotic DNATopoisomersase I.
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Cleavage of DNA by mammalian DNA topoisomerase II.
TL;DR: Detailed characterization of the cleavage products has revealed that topoisomerase II cuts DNA with a four-base stagger and is covalently linked to the protruding 5'-phosphoryl ends of each broken DNA strand.
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Isolation and genetic characterization of human KB cell lines resistant to multiple drugs.
TL;DR: In this paper, human KB cell lines resistant to high levels of colchicine were isolated by several successive single-step selections, which resulted in cross-resistance to vincristine, vinblastine, adriamycin, actinomycin D, and puromycin.