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Angew Chem Int Ed Engl. 2011 Oct 10;50(42):9832-7. doi: 10.1002/anie.201102965. Epub 2011 Sep 9.

Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design.

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1
Max-Planck-Institut für molekulare Physiologie, Abt. Chemische Biologie, Dortmund, Germany.

Abstract

A matter of common sense: a common recognition motif consisting of a negatively charged group five to six bonds away (red) from the (thio)ester functionality (green) and a positively charged tail group ten to twelve bonds away (blue) was identified in two native acyl protein thioesterase 1 (APT1) substrates. This similarity led to the design of potent inhibitors of the Ras-depalmitoylating enzyme APT1.

PMID:
21905185
DOI:
10.1002/anie.201102965
[Indexed for MEDLINE]
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