Nick-containing oligonucleotides as human topoisomerase I inhibitors

被引：6

作者：

Chua, Sock Teng ^{[1
]}

Quek, Ngee Mien ^{[1
]}

Li, Ming ^{[1
]}

Ng, Magdeline Tao Tao ^{[1
]}

Yuan, Weixing ^{[1
]}

Chua, May Ling ^{[1
]}

Guo, Juanjuan ^{[1
]}

Koh, Li Eng ^{[1
]}

Ye, Ruijuan ^{[1
]}

Li, Tianhu ^{[1
]}

机构：

[1] Nanyang Technol Univ, Div Chem & Biol Chem, Sch Phys & Math Sci, Singapore 637616, Singapore

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期

关键词：

Human topoisomerase I; Enzyme inhibitor; Stable hairpins; Nick oligonucleotides; DNA TOPOISOMERASES; CIRCULAR OLIGONUCLEOTIDES; CAMPTOTHECINS; MECHANISM; CLEAVAGE; PROGRESS; PROTEIN; ROLES; DRUGS;

D O I：

10.1016/j.bmcl.2008.12.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 IC50 value of 6.3 nM. Our studies have also demonstrated that the position of the nick as well as the length of the oligonucleotides were crucial factors for the inhibition of this nuclear enzyme. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：618 / 623

页数：6

共 23 条

[1]

[Anonymous], 2003, AAPS NEWSMAG

[2] Inhibition of Mycobacterium smegmatis topoisomerase I by specific oligonucleotides [J].

Bhaduri, T ;

Basak, S ;

Sikder, D ;

Nagaraja, V .

FEBS LETTERS, 2000, 486 (02) :126-130

[3] Interaction of human DNA topoisomerase I with specific sequence oligodeoxynucleotides [J].

Bugreev, DV ;

Vasyutina, EL ;

Kolocheva, TI ;

Buneva, VN ;

Andoh, T ;

Nevinsky, GA .

BIOCHIMIE, 1998, 80 (04) :303-308

[4] DNA topoisomerases: Structure, function, and mechanism [J].

Champoux, JJ .

ANNUAL REVIEW OF BIOCHEMISTRY, 2001, 70 :369-413

[5]

CHRISTIANSEN K, 1993, J BIOL CHEM, V268, P9690

[6] Structure, molecular mechanisms, and evolutionary relationships in DNA topoisomerases [J].

Corbett, KD ;

Berger, JM .

ANNUAL REVIEW OF BIOPHYSICS AND BIOMOLECULAR STRUCTURE, 2004, 33 :95-118

[7] An overview of progress in antisense therapeutics [J].

Crooke, ST .

ANTISENSE & NUCLEIC ACID DRUG DEVELOPMENT, 1998, 8 (02) :115-122

[8]

HUSAIN I, 1994, CANCER RES, V54, P539

[9] Human DNA topoisomerase I: relaxation, roles, and damage control [J].

Leppard, JB ;

Champoux, JJ .

CHROMOSOMA, 2005, 114 (02) :75-85

[10]

LI CJ, 1993, J BIOL CHEM, V268, P22463

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