Drugs targeting synaptic RNA m6A methylation regulate synaptic transmission and plasticity in the rat hippocampus

m6A methylation is the most abundant modification in eukaryotic mRNA and has been implicated in epitranscriptomic regulation of various cellular functions. Recent studies have demonstrated its significance in brain development, neuronal signalling and memory formation; however, the precise mechanisms by which m6A RNA methylation affects synaptic transmission and plasticity in memory-related neuronal circuits remain unclear. Here, we have studied the effects of newly developed pharmacological compounds that target m6A methylation on excitatory synaptic transmission and plasticity in the hippocampus, using a combination of electrophysiological and immunohistological techniques in infant and adult rats. We demonstrate that STM2457, a highly potent catalytic inhibitor of the m6A methyltransferase METTL3, blocks long-term potentiation (LTP) without affecting basal synaptic transmission in area CA1. Moreover, our findings support that LTP in vivo is associated with elevated m6A immunostaining, suggesting that LTP induction triggers METTL3 activation and a subsequent rise in m6A methylation. Interestingly, pharmacological activation of METTL3/14 or inhibition of the m6A demethylase FTO increased synaptic m6A levels in vivo, yet attenuated LTP in adult hippocampal slices. METTL3/14 activation also diminished long-term depression (LTD). These findings align with a model where elevated m6A methylation acts as a stabilizing signal, limiting excessive activity-dependent plasticity of synaptic transmission across development. Furthermore, they add to the growing body of evidence supporting that dysregulation of m6A RNA methylation perturbs synaptic plasticity - the neurobiological foundation of memory - and demonstrate that these processes can be pharmacologically targeted.

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Publication Details

Journal
Experimental Neurology
Published
2026-04-30
DOI
https://doi.org/10.1016/j.expneurol.2026.115802
Primary Topic
RNA modifications and cancer
Type
article
Field-Weighted Citation Impact
0.00

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article

Drugs targeting synaptic RNA m6A methylation regulate synaptic transmission and plasticity in the rat hippocampus

Indrek Teino, Jun Kyu Rhee, Brunaldo Renzi, M Saarma et al.
Experimental Neurology
RNA modifications and cancer
article

Drugs targeting synaptic RNA m6A methylation regulate synaptic transmission and plasticity in the rat hippocampus

Indrek Teino, Jun Kyu Rhee, Brunaldo Renzi, M Saarma, Rahaf Keskinen, Sari E Lauri
article en

Abstract

m6A methylation is the most abundant modification in eukaryotic mRNA and has been implicated in epitranscriptomic regulation of various cellular functions. Recent studies have demonstrated its significance in brain development, neuronal signalling and memory formation; however, the precise mechanisms by which m6A RNA methylation affects synaptic transmission and plasticity in memory-related neuronal circuits remain unclear. Here, we have studied the effects of newly developed pharmacological compounds that target m6A methylation on excitatory synaptic transmission and plasticity in the hippocampus, using a combination of electrophysiological and immunohistological techniques in infant and adult rats. We demonstrate that STM2457, a highly potent catalytic inhibitor of the m6A methyltransferase METTL3, blocks long-term potentiation (LTP) without affecting basal synaptic transmission in area CA1. Moreover, our findings support that LTP in vivo is associated with elevated m6A immunostaining, suggesting that LTP induction triggers METTL3 activation and a subsequent rise in m6A methylation. Interestingly, pharmacological activation of METTL3/14 or inhibition of the m6A demethylase FTO increased synaptic m6A levels in vivo, yet attenuated LTP in adult hippocampal slices. METTL3/14 activation also diminished long-term depression (LTD). These findings align with a model where elevated m6A methylation acts as a stabilizing signal, limiting excessive activity-dependent plasticity of synaptic transmission across development. Furthermore, they add to the growing body of evidence supporting that dysregulation of m6A RNA methylation perturbs synaptic plasticity - the neurobiological foundation of memory - and demonstrate that these processes can be pharmacologically targeted.

Experimental NeurologyVol. 402
University of Helsinki (FI)
Academy of Finland, Suomen Kulttuurirahasto, Sigrid Juséliuksen Säätiö, Novo Nordisk Fonden
Good health and well-being
Openalex Percentile: Top 12%
RNA modifications and cancer
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