Target intelligence / Profile preview

RNA methyltransferase

Molecular classification
Enzyme, Class I methyltransferase (Rossmann-fold domain), Class IV methyltransferase (SPOUT domain)
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Overview

RNA methyltransferase refers to a group of enzymes that mediate methyl group addition to RNA molecules, mainly using S-adenosyl-L-methionine (SAM) as a methyl donor. These enzymes recognize specific RNA substrates (e.g., mRNA, tRNA, rRNA), modifying nucleotides at distinct positions such as N6-adenosine (m^6A), 2’-O-ribose, or m^7G cap structures. Well-characterized families include METTL (Methyltransferase-like proteins, e.g., METTL3, METTL16), NSUN (NOP2/Sun), and TRMT (tRNA methyltransferase subfamilies). RNA methyltransferases are essential for epigenetic gene regulation, cell differentiation, RNA stability, and have been implicated in diverse pathologies including cancers and viral infections. Inhibitors of RNA methyltransferases are being investigated for therapeutic use, though clinical candidates are still emerging.

Other names
RNA MTaseMethyltransferase-like protein (e.g., METTL)tRNA methyltransferase (TRMT)NOP2/Sun RNA methyltransferase (NSUN)2’-O-methyltransferase (2’-O-MTase)N6-adenosine methyltransferase
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Mechanism of action

Inhibition of methyl group transfer to RNA nucleotides (reducing mRNA/tRNA modification) Modulation of RNA stability and translation Suppression of viral replication (by targeting viral MTases)

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Biological functions

RNA modification (methylation)Regulation of gene expressionEpigenetic controlRNA stability and processingCell differentiation and development
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Disease associations

CancerInfection (notably antiviral, e.g., coronaviruses)Neurodevelopmental disordersOther (multiple cellular pathologies via RNA dysregulation)
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Safety considerations

Broad inhibition may disrupt normal RNA metabolism leading to off-target effectsPotential for cytotoxicity, immune dysregulation, or impact on cell cycle and differentiation
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Interacting drugs

Small molecule inhibitors are under development

2 more in the full profile.

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Biomarkers

Levels of specific RNA methylation marks (e.g., m^6A, 2’-O-methylation, m^7G) in cancer or viral infectionExpression of specific MTase genes (e.g., METTL1, METTL3)

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