Abstract
Inhibition of Bcl2 family proteins Bcl-X(L) and Bcl-2 represents a promising drug development strategy for cancer treatment by triggering apoptosis in cancer cells. Here we report a novel Bcl-X(L) inhibitor, Z36, which unexpectedly induces only autophagic cell death, but not apoptosis. This special property distinguishes Z36 from other previously reported Bcl-X(L) and Bcl-2 inhibitors that induce cancer cell death mainly through apoptosis, and makes Z36 an attractive molecular tool for studying the cellular regulation of autophagic cell death and apoptosis.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine / analogs & derivatives
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Adenine / metabolism
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Antineoplastic Agents / pharmacology
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Autophagy*
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Dose-Response Relationship, Drug
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Green Fluorescent Proteins / metabolism
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HeLa Cells
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Humans
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Indoles / pharmacology*
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Microscopy, Electron, Transmission
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Models, Chemical
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Molecular Conformation
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Proto-Oncogene Proteins c-bcl-2 / metabolism*
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RNA Interference
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RNA, Small Interfering / metabolism
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Surface Plasmon Resonance
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bcl-X Protein / antagonists & inhibitors*
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bcl-X Protein / biosynthesis*
Substances
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5-fluoro-1-(3'-dimethylamino)propyl-indolin-2-one
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Antineoplastic Agents
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Indoles
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Proto-Oncogene Proteins c-bcl-2
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RNA, Small Interfering
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bcl-X Protein
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Green Fluorescent Proteins
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3-methyladenine
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Adenine