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Article

Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets.

Structure (London, England : 1993) - 3 May 2016

Van Aller Glenn S, Graves Alan P, Elkins Patricia A, Bonnette William G, McDevitt Patrick J, Zappacosta Francesca, Annan Roland S, Dean Tony W, Su Dai-Shi, Carpenter Christopher L, Mohammad Helai P, Kruger Ryan G

Abstract excerpt

SMYD3 is a lysine methyltransferase overexpressed in colorectal, breast, prostate, and hepatocellular tumors, and has been implicated as an oncogene in human malignancies. Methylation of MEKK2 by SMYD3 is important for regulation of the MEK/ERK pathway, suggesting the possibility of selectively targeting SMYD3 in RAS-driven cancers. Structural and kinetic characterization of SMYD3 was undertaken leading to a...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

Identifiers

PMID: 27066749
DOI: 10.1016/j.str.2016.03.010

Genes

SMYD3

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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