Abstract
Protein prenyl transferases have been a focus of anti-cancer drug discovery in recent years due to their roles in post-translational modification of small GTP binding proteins. Attention is now turning to the development of GGTase I inhibitors. Here, we present the synthesis and biological evaluation of four GGPP analogs versus mammalian GGTase I and the discovery that 7-allyl GGPP is a surprisingly efficient GGTase I substrate.
Publication types
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Evaluation Study
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Animals
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Farnesyltranstransferase / antagonists & inhibitors*
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Humans
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Magnetic Resonance Spectroscopy
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Mice
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Molecular Structure
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Polyisoprenyl Phosphates / chemical synthesis*
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Polyisoprenyl Phosphates / pharmacology*
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Protein Prenylation
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Protein Processing, Post-Translational
Substances
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Polyisoprenyl Phosphates
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Alkyl and Aryl Transferases
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geranylgeranyltransferase type-I
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Farnesyltranstransferase
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geranylgeranyl pyrophosphate