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.
authors.affiliation: Laboratory for Translational Research, Harvard Medical School, Cambridge, MA 02139, USA. yunhuafan@yahoo.com
authors.forename: Yun-Hua
authors.initials: YH
authors.lastname: Fan
authors.forename: Han
authors.initials: H
authors.lastname: Chen
authors.forename: Amarnath
authors.initials: A
authors.lastname: Natarajan
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Guo
authors.forename: Fred
authors.initials: F
authors.lastname: Harbinski
authors.forename: Julia
authors.initials: J
authors.lastname: Iyasere
authors.forename: William
authors.initials: W
authors.lastname: Christ
authors.forename: Huseyin
authors.initials: H
authors.lastname: Aktas
authors.forename: Jose A
authors.initials: JA
authors.lastname: Halperin
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002839:Chromans / Q000138:chemical synthesis / Q000494:pharmacology*; D015852:Eukaryotic Initiation Factor-2 / Q000378:metabolism; D006801:Humans; D010766:Phosphorylation / Q000187:drug effects; D014176:Protein Biosynthesis / Q000187:drug effects; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000494:pharmacology*; D000077288:Troglitazone
chemical_list: D000970:Antineoplastic Agents; D002839:Chromans; D015852:Eukaryotic Initiation Factor-2; D045162:Thiazolidinediones; D000077288:Troglitazone; D002118:Calcium