Inhibition of telomerase by BIBR 1532 and related analogues

D. K. Barma; Anissa Elayadi; J R Falck; David R Corey

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

Inhibition of telomerase by BIBR 1532 and related analogues

D. K. Barma, Anissa Elayadi, J R Falck, David R Corey

Research output: Contribution to journal › Article › peer-review

43 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1333-1336
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	7
DOIs	https://doi.org/10.1016/S0960-894X(03)00101-X
State	Published - Apr 7 2003

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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

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title = "Inhibition of telomerase by BIBR 1532 and related analogues",

abstract = "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.",

author = "Barma, {D. K.} and Anissa Elayadi and Falck, {J R} and Corey, {David R}",

note = "Funding Information: Supported financially by the Robert A. Welch Foundation (I-1244 and GL625910) and grants from the National Institutes of Health GM31278, CA 85363 and CA70907. We thank Becky McKinney for skilled assistance with telomerase assay. ",

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AU - Barma, D. K.

AU - Elayadi, Anissa

AU - Falck, J R

AU - Corey, David R

N1 - Funding Information: Supported financially by the Robert A. Welch Foundation (I-1244 and GL625910) and grants from the National Institutes of Health GM31278, CA 85363 and CA70907. We thank Becky McKinney for skilled assistance with telomerase assay.

PY - 2003/4/7

Y1 - 2003/4/7

N2 - 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.

AB - 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.

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Inhibition of telomerase by BIBR 1532 and related analogues

Abstract

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