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A combinatorial approach to characterize the substrate specificity of protein arginine methyltransferase 1.


ABSTRACT: The dysregulation of protein arginine methyltransferases (PRMTs) is implicated in a wide variety of disease states. Here we report the design, synthesis, and screening of a combinatorial peptide library used to characterize the substrate specificity of PRMT1. The information gained from this approach was used to develop a PRMT1 inhibitor with enhanced selectivity.

SUBMITTER: Bicker KL 

PROVIDER: S-EPMC2999663 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature

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A combinatorial approach to characterize the substrate specificity of protein arginine methyltransferase 1.

Bicker Kevin L KL   Obianyo Obiamaka O   Rust Heather L HL   Thompson Paul R PR  

Molecular bioSystems 20100706 1


The dysregulation of protein arginine methyltransferases (PRMTs) is implicated in a wide variety of disease states. Here we report the design, synthesis, and screening of a combinatorial peptide library used to characterize the substrate specificity of PRMT1. The information gained from this approach was used to develop a PRMT1 inhibitor with enhanced selectivity. ...[more]

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