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<p>Kainate receptors are a subtype of ionotropic glutamate receptors. Potent and selective modulatory agents of kainate receptors are potential drug candidates for treatment of various neurological diseases involving receptor dysregulation. Here, we report an RNA aptamer that selectively potentiates GluK2, a key kainate receptor subunit. The potentiating aptamer, termed U9, is designed by changing the sequence of the predecessor RNA, which is an inhibitor without subunit selectivity, leading to the change of function: U9 selectively potentiates GluK2 with an EC<sub>50</sub> of ~ 210 nM. Our study demonstrates a potential utility of combining molecular docking with functional assay for a template-based discovery of potent, single-subunit selective RNA aptamers.</p>

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GluK2 kainate receptor subunit-selective, potentiating RNA aptamer

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年9月11日

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  • Samantha R. Ingenito,
  • Noah Saunders,
  • Kyle J. Lininger,
  • Li Niu

摘要

Kainate receptors are a subtype of ionotropic glutamate receptors. Potent and selective modulatory agents of kainate receptors are potential drug candidates for treatment of various neurological diseases involving receptor dysregulation. Here, we report an RNA aptamer that selectively potentiates GluK2, a key kainate receptor subunit. The potentiating aptamer, termed U9, is designed by changing the sequence of the predecessor RNA, which is an inhibitor without subunit selectivity, leading to the change of function: U9 selectively potentiates GluK2 with an EC50 of ~ 210 nM. Our study demonstrates a potential utility of combining molecular docking with functional assay for a template-based discovery of potent, single-subunit selective RNA aptamers.