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Controlling gene expression by zinc(II)–macrocyclic tetraamine complexes by Emiko Kikuta; Tohru Koike; Eiichi Kimura is a Chemistry article available to read on EtoBox.

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The zinc(II) complexes of 12-membered macrocyclic tetraamines (1,4,7,10-tetraazacyclododecane, cyclen) appended with one or two aryl-methyl group(s) (quinolyl-methyl, naphthyl-methyl, and acridinyl-methyl) selectively bind to thymines in a TATA box of the SV40 early promoter region and thus inhibit the binding of a transcriptional factor, TATA binding protein. These Zn 2q -cyclen derivatives also act as inhibitors of DNA-targeted enzymes, type I and type II topoisomerases. They also exhibited strong antimicrobial activities for the Grampositive bacterial strain. These biochemical and biological properties were compared with those of conventionally established AT-recognizing drugs, distamycin A and DAPI. The Zn 2q -cyclen complexes are a new type of small molecular, genetic transcriptional regulation factor.

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Author

Emiko Kikuta; Tohru Koike; Eiichi Kimura

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0162-0134)

Published

2000

Language

EN

Field

Chemistry (Physical Sciences)