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Inhibition of Unwinding of G-quadruplex Structures by Sgs1 Helicase in the Presence of N,N'-bis[2-(1-piperidino)ethyl]-3,4,9,10-perylenetetracarboxylic Diimide, a G-quadruplex-interactive Ligand

Inhibition of Unwinding of G-quadruplex Structures by Sgs1 Helicase in the Presence of N,N'-bis[2-(1-piperidino)ethyl]-3,4,9,10-perylenetetracarboxylic Diimide, a G-quadruplex-interactive Ligand

H Han, R J Bennett, L H Hurley

Biochemistry. 2000 Aug 8;39(31):9311-6.

PMID: 10924124

Abstract:

N,N'-Bis[2-(1-piperidino)ethyl]-3,4,9,10-perylenetetracarboxylic diimide (PIPER), a perylene derivative, is a very potent and selective G-quadruplex DNA-interactive agent. It has been shown to inhibit DNA polymerase and telomerase by stacking externally to the G-tetrads in the G-quadruplex structures. Recently, we have demonstrated that this small molecule greatly accelerates the assembly of G-quadruplex structures in a cell-free system. In this report, we present data demonstrating that PIPER prevents the unwinding of G-quadruplex structures by yeast Sgs1 helicase. Sgs1 belongs to the RecQ DNA helicase family whose members include other G-quadruplex DNA unwinding helicases, such as human Bloom's syndrome and human Werner's syndrome helicases. PIPER specifically prevents the unwinding of G-quadruplex DNA but not duplex DNA by Sgs1. Competition experiments indicate that this inhibitory activity is due to the interaction of PIPER with G-quadruplex structures rather than the helicase itself. These results combined with previous studies suggest a possible mechanism of action for these G-quadruplex-interactive agents inside cells: they might induce G-quadruplex formation in G-rich regions on genomic DNA, stabilize these structures, and prevent them from being cleared by enzymes such as helicases. The G-quadruplex structures may, in turn, disrupt some critical cellular events such as DNA replication, transcription regulation, and telomere maintenance.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP215297180	N,N′-Bis[2-(2-tert-butyldimethylsilyloxyethoxy)ethyl]-3,4,9,10-perylenetetracarboxylic diimide		215297-18-0	Price

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