Inhibition of telomerase by BIBR 1532 and related analogues

被引：37

作者：

Barma, DK

Elayadi, A

Falck, JR

Corey, DR

机构：

[1] Univ Texas, SW Med Ctr Dallas, Dept Pharmacol, Dallas, TX 75390 USA

[2] Univ Texas, SW Med Ctr Dallas, Dept Biochem, Dallas, TX 75390 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00101-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

BIBR 1532 has been reported to be a potent, small molecule inhibitor of human telomerase, suggesting it as a lead for the development of anti-telomerase therapy. We confirm the ability of BIBR 1532 to inhibit telomerase and report the discovery of an equally potent analogue. Importantly, IC50 values in cell extract are considerably higher than those previously reported using assays for purified enzyme, indicating that substantial improvement may be necessary. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1333 / 1336

页数：4

共 27 条

[1] Novel antisense and peptide nucleic acid strategies for controlling gene expression [J].

Braasch, DA ;

Corey, DR .

BIOCHEMISTRY, 2002, 41 (14) :4503-4510

[2] TELOMERASE ACTIVITY IN HUMAN OVARIAN-CARCINOMA [J].

COUNTER, CM ;

HIRTE, HW ;

BACCHETTI, S ;

HARLEY, CB .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (08) :2900-2904

[3] A highly selective telomerase inhibitor limiting human cancer cell proliferation [J].

Damm, K ;

Hemmann, U ;

Garin-Chesa, P ;

Hauel, N ;

Kauffmann, I ;

Priepke, H ;

Niestroj, C ;

Daiber, C ;

Enenkel, B ;

Guilliard, B ;

Lauritsch, I ;

Müller, E ;

Pascolo, E ;

Sauter, G ;

Pantic, M ;

Martens, UM ;

Wenz, C ;

Lingner, J ;

Kraut, N ;

Rettig, WJ ;

Schnapp, A .

EMBO JOURNAL, 2001, 20 (24) :6958-6968

[4] Inhibition of telomerase by 2′-O-(2-methoxyethyl) RNA oligomers:: effect of length, phosphorothioate substitution and time inside cells [J].

Elayadi, AN ;

Demieville, A ;

Wancewicz, EV ;

Monia, BP ;

Corey, DR .

NUCLEIC ACIDS RESEARCH, 2001, 29 (08) :1683-1689

[5] THE RNA COMPONENT OF HUMAN TELOMERASE [J].

FENG, JL ;

FUNK, WD ;

WANG, SS ;

WEINRICH, SL ;

AVILION, AA ;

CHIU, CP ;

ADAMS, RR ;

CHANG, E ;

ALLSOPP, RC ;

YU, JH ;

LE, SY ;

WEST, MD ;

HARLEY, CB ;

ANDREWS, WH ;

GREIDER, CW ;

VILLEPONTEAU, B .

SCIENCE, 1995, 269 (5228) :1236-1241

[6]

Gürtler C, 1999, CHEM-EUR J, V5, P3107, DOI 10.1002/(SICI)1521-3765(19991105)5:11<3107::AID-CHEM3107>3.0.CO

[7]

2-#

[8] Creation of human tumour cells with defined genetic elements [J].

Hahn, WC ;

Counter, CM ;

Lundberg, AS ;

Beijersbergen, RL ;

Brooks, MW ;

Weinberg, RA .

NATURE, 1999, 400 (6743) :464-468

[9] TELOMERES SHORTEN DURING AGING OF HUMAN FIBROBLASTS [J].

HARLEY, CB ;

FUTCHER, AB ;

GREIDER, CW .

NATURE, 1990, 345 (6274) :458-460

[10] Human telomerase contains evolutionarily conserved catalytic and structural subunits [J].

Harrington, L ;

Zhou, W ;

McPhail, T ;

Oulton, R ;

Yeung, DSK ;

Mar, V ;

Bass, MB ;

Robinson, MO .

GENES & DEVELOPMENT, 1997, 11 (23) :3109-3115

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