A new type of AT‐specific ligand constructed of two netropsin‐like molecules

Khorlin, A.A.; Крылов, А. С.; Grokhovsky, S. L.; Zhuze, A. L.; Заседателев, А. С.; Gursky, G. V.; Gottikh, B. P.

doi:10.1016/0014-5793(80)80246-8

Cited by 41 publications

(21 citation statements)

References 8 publications

(2 reference statements)

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“…This has unfortunate consequences for polyto-head, with N-terminus connected to N-terminus through a hydrocarbon linker, were created to target amide design: in longer polyamides, the amide groups get out of phase with the DNA bases, limiting longer AT-rich sequences. 18 …”

Section: Phasing Incompatibilitymentioning

confidence: 97%

Progress in the design of DNA sequence-specific lexitropsins

Walker¹,

Kopka²,

Goodsell³

1997

Biopolymers

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Sequence‐specific polyamides that bind in the minor groove of DNA are attractive candidates for antibiotics, cancer chemotherapeutics, and transcriptional antagonists. This paper reviews the progress of structure‐based design of minor‐groove‐binding polyamides, from the first structure of netropsin with DNA, to the effective linked polyamides currently under study. A theory of polyamide specificity is also reviewed, introducing methods to determine the optimal strategies for targeting a given DNA sequence within a genome of competing sequences. © 1998 John Wiley & Sons, Inc. Biopoly 44: 323–334, 1997

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Section: Phasing Incompatibilitymentioning

confidence: 97%

Progress in the design of DNA sequence-specific lexitropsins

Walker¹,

Kopka²,

Goodsell³

1997

Biopolymers

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“…Since each of Nt subunits may separately bind DNA, the bis-Nts are capable of bidendate interaction with DNA [13,14,20]. It is reasonable to assume that the ligands which arc able to bind specifically to longer stretches of DNA in the minor groove should be more potent topo I inhibitors.…”

Section: Discussionmentioning

confidence: 99%

“…In our previous studies we synthesized a seria of high sequence-specific derivatives ofbis-Nts [11,12] and analyzed their ability to bind DNA and to inhibit a number of DNA-directed enzymes [13][14][15]. The choice of these bis-Nt derivatives ( The present paper describes the effects of this new seria ofbis-Nts capable of bidendate binding to DNA (Fig.…”

Section: Introductionmentioning

confidence: 99%

Human DNA‐topoisomerase I activity is affected by bis‐netropsin's binding to DNA minor groove

et al. 1998

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SUMMARYBis-netropsins (bis-Nts) are known to be efficient inhibitors of human DNA topoisomerase (topo) I with a higher antitumor activity than netropsin. New sequence-specific derivatives of bis-Nts were used for modulation of topo I-mediated DNA cleavage with and without camptothecin (CPT). Relation between the bis-Nts binding sites and topo I cleavage sites has been analyzed with the plasmid DNA constructs generated by insertion of synthetic oligonucleotides containing various topo I-cleavage and bis-Nt-binding sites. These constructs offer an opportunity to study minor groove binders effects on the topo I reaction on DNA. Three major effects: (i) bis-Nt -mediated disappearance of some of the topo I cleavage sites; (ii) enhancement of some other sites, and, (iii) generation of new cleavage sites, have been found and analyzed. These effects demonstrate that bis-Nts drastically change the topo Imediated DNA cleavage.

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“…Earlier, we synthesized a number of new netropsin (Nt) derivatives that appeared to be highly selective inhibitors of herpesvirus type 1 (HV-1) reproduction, including drug-resistant variants [1][2][3][4][5].…”

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confidence: 99%