N-(1-Pyrenyl) maleimide inhibits telomerase activity in a cell free system and induces apoptosis in Jurkat cells

Pei Rong Huang; Yuan Ming Yeh; Chia Chu Pao; Chi Yuan Chen; Tzu Chien V. Wang

doi:10.1007/s11033-012-1757-y

N-(1-Pyrenyl) maleimide inhibits telomerase activity in a cell free system and induces apoptosis in Jurkat cells

Pei Rong Huang, Yuan Ming Yeh, Chia Chu Pao, Chi Yuan Chen, Tzu Chien V. Wang^*

^*Corresponding author for this work

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

12 Scopus citations

Abstract

Telomerase activity is repressed in normal human somatic cells, but is activated in most cancers, suggesting that telomerase may be an important target for cancer therapy. Agents that interact selectively with telomerase are anticipated to exert specific action on cancer cells. In this study, we evaluated maleimide derivatives for their potency and selectivity of telomerase inhibition. Among the several N-substituted derivatives of maleimide tested, N-(1-Pyrenyl) maleimide was shown to exert the greatest inhibition of telomerase in a cell free system, with an IC50 value of 0.25 μM. Importantly, we demonstrated that N-(1-pyrenyl) maleimide induces apoptosis in Jurkat T cells and displays the greatest differential cytotoxicity against hematopoietic cancer cells. These results suggest that N-(1-pyrenyl) maleimide is an attractive maleimide to be tested and developed as anti-cancer drug.

Original language	English
Pages (from-to)	8899-8905
Number of pages	7
Journal	Molecular Biology Reports
Volume	39
Issue number	9
DOIs	https://doi.org/10.1007/s11033-012-1757-y
State	Published - 09 2012

Keywords

Apoptosis
Maleimides
N-(1-Pyrenyl) maleimide
Telomerase inhibitor

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1007/s11033-012-1757-y

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title = "N-(1-Pyrenyl) maleimide inhibits telomerase activity in a cell free system and induces apoptosis in Jurkat cells",

abstract = "Telomerase activity is repressed in normal human somatic cells, but is activated in most cancers, suggesting that telomerase may be an important target for cancer therapy. Agents that interact selectively with telomerase are anticipated to exert specific action on cancer cells. In this study, we evaluated maleimide derivatives for their potency and selectivity of telomerase inhibition. Among the several N-substituted derivatives of maleimide tested, N-(1-Pyrenyl) maleimide was shown to exert the greatest inhibition of telomerase in a cell free system, with an IC50 value of 0.25 μM. Importantly, we demonstrated that N-(1-pyrenyl) maleimide induces apoptosis in Jurkat T cells and displays the greatest differential cytotoxicity against hematopoietic cancer cells. These results suggest that N-(1-pyrenyl) maleimide is an attractive maleimide to be tested and developed as anti-cancer drug.",

keywords = "Apoptosis, Maleimides, N-(1-Pyrenyl) maleimide, Telomerase inhibitor",

author = "Huang, {Pei Rong} and Yeh, {Yuan Ming} and Pao, {Chia Chu} and Chen, {Chi Yuan} and Wang, {Tzu Chien V.}",

year = "2012",

month = sep,

doi = "10.1007/s11033-012-1757-y",

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journal = "Molecular Biology Reports",

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TY - JOUR

T1 - N-(1-Pyrenyl) maleimide inhibits telomerase activity in a cell free system and induces apoptosis in Jurkat cells

AU - Huang, Pei Rong

AU - Yeh, Yuan Ming

AU - Pao, Chia Chu

AU - Chen, Chi Yuan

AU - Wang, Tzu Chien V.

PY - 2012/9

Y1 - 2012/9

N2 - Telomerase activity is repressed in normal human somatic cells, but is activated in most cancers, suggesting that telomerase may be an important target for cancer therapy. Agents that interact selectively with telomerase are anticipated to exert specific action on cancer cells. In this study, we evaluated maleimide derivatives for their potency and selectivity of telomerase inhibition. Among the several N-substituted derivatives of maleimide tested, N-(1-Pyrenyl) maleimide was shown to exert the greatest inhibition of telomerase in a cell free system, with an IC50 value of 0.25 μM. Importantly, we demonstrated that N-(1-pyrenyl) maleimide induces apoptosis in Jurkat T cells and displays the greatest differential cytotoxicity against hematopoietic cancer cells. These results suggest that N-(1-pyrenyl) maleimide is an attractive maleimide to be tested and developed as anti-cancer drug.

AB - Telomerase activity is repressed in normal human somatic cells, but is activated in most cancers, suggesting that telomerase may be an important target for cancer therapy. Agents that interact selectively with telomerase are anticipated to exert specific action on cancer cells. In this study, we evaluated maleimide derivatives for their potency and selectivity of telomerase inhibition. Among the several N-substituted derivatives of maleimide tested, N-(1-Pyrenyl) maleimide was shown to exert the greatest inhibition of telomerase in a cell free system, with an IC50 value of 0.25 μM. Importantly, we demonstrated that N-(1-pyrenyl) maleimide induces apoptosis in Jurkat T cells and displays the greatest differential cytotoxicity against hematopoietic cancer cells. These results suggest that N-(1-pyrenyl) maleimide is an attractive maleimide to be tested and developed as anti-cancer drug.

KW - Apoptosis

KW - Maleimides

KW - N-(1-Pyrenyl) maleimide

KW - Telomerase inhibitor

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U2 - 10.1007/s11033-012-1757-y

DO - 10.1007/s11033-012-1757-y

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SN - 0301-4851

VL - 39

SP - 8899

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JO - Molecular Biology Reports

JF - Molecular Biology Reports

IS - 9

ER -

N-(1-Pyrenyl) maleimide inhibits telomerase activity in a cell free system and induces apoptosis in Jurkat cells

Abstract

Keywords

UN SDGs

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