Target intelligence / Profile preview

SET and MYND domain-containing protein 3 (SMYD3)

Target
SMYD3
Molecular classification
Enzyme, Histone modification enzyme, Transcription factor co-regulator
01

Overview

SET and MYND domain-containing protein 3 (SMYD3) is a lysine methyltransferase enzyme encoded by the SMYD3 gene in humans[1]. It catalyzes the methylation of specific lysine residues on histones H3 (H3K4) and H4 (H4K5), thus facilitating transcriptional activation by promoting chromatin remodeling and recruitment of RNA polymerase II[1]. SMYD3 plays a notable role in cancer progression, being overexpressed in several cancer types (including liver, breast, colorectal, lung, esophageal, and prostate cancers), where it can promote oncogenic signaling by regulating gene expression and the MAPK pathway[1]. SMYD3 is predominantly expressed in skeletal muscle and testis[1]. It acts as a transcriptional co-regulator by regulating chromatin structure and has been implicated as a promising therapeutic target in oncology and vascular senescence[2].

Other names
SMYD3SET and MYND domain containing 3
02

Mechanism of action

Histone methyltransferase inhibition, Disruption of MAPK pathway signaling

03

Biological functions

Histone lysine methylationTranscriptional regulationEpigenetic regulationSignal transduction
04

Disease associations

CancerVascular senescence
05

Safety considerations

Potential for effect on normal gene expression and epigenetic regulation
06

Biomarkers

SMYD3 overexpression for certain cancers (selection)

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