Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

Yun Hua Fan; Han Chen; Amarnath Natarajan; Yuhong Guo; Fred Harbinski; Julia Iyasere; William Christ; Huseyin Aktas; Jose A. Halperin

doi:10.1016/j.bmcl.2004.02.087

Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

Yun Hua Fan, Han Chen, Amarnath Natarajan, Yuhong Guo, Fred Harbinski, Julia Iyasere, William Christ, Huseyin Aktas, Jose A. Halperin

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

47 Scopus citations

Abstract

Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.

Original language	English (US)
Pages (from-to)	2547-2550
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2004.02.087
State	Published - May 17 2004
Externally published	Yes

Keywords

Intracellular calcium
Thiazolidinediones
Troglitazone

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2004.02.087

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title = "Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium",

abstract = "Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.",

keywords = "Intracellular calcium, Thiazolidinediones, Troglitazone",

author = "Fan, {Yun Hua} and Han Chen and Amarnath Natarajan and Yuhong Guo and Fred Harbinski and Julia Iyasere and William Christ and Huseyin Aktas and Halperin, {Jose A.}",

note = "Funding Information: The authors wish to thank Drs. Daniel C. Tosteson and Magdalena Tosteson for their continuous support. In addition, we thank Dr. Michael Chorev for his comments and discussion. These studies were supported in part by NIH National Cooperative Drug Discovery Group (NCDDG) grant U19 CA87427 and NIH CA78411. ",

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AU - Fan, Yun Hua

AU - Chen, Han

AU - Natarajan, Amarnath

AU - Guo, Yuhong

AU - Harbinski, Fred

AU - Iyasere, Julia

AU - Christ, William

AU - Aktas, Huseyin

AU - Halperin, Jose A.

N1 - Funding Information: The authors wish to thank Drs. Daniel C. Tosteson and Magdalena Tosteson for their continuous support. In addition, we thank Dr. Michael Chorev for his comments and discussion. These studies were supported in part by NIH National Cooperative Drug Discovery Group (NCDDG) grant U19 CA87427 and NIH CA78411.

PY - 2004/5/17

Y1 - 2004/5/17

N2 - Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.

AB - Depletion of calcium from the endoplasmic reticulum has shown to affect protein synthesis and cell proliferation. The anticancer effect of troglitazone was reported to be mediated by depletion of intracellular calcium stores resulting in inhibition of translation initiation. The unsaturated form of troglitazone displays similar anticancer properties in vitro. In this letter, we report our findings on the minimum structural requirements for both compounds to retain their calcium release and antiproliferative activities.

KW - Intracellular calcium

KW - Thiazolidinediones

KW - Troglitazone

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Structure-activity requirements for the antiproliferative effect of troglitazone derivatives mediated by depletion of intracellular calcium

Abstract

Keywords

ASJC Scopus subject areas

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