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Synapse
June 28, 20260 citations

Structure-guided development of a potent human B0AT1 inhibitor effective in a mouse model of phenylketonuria.

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TITakuya ImazuTATomoya AkashiMHMasahiro Hiraizumi

Key Points

  • The aim is to develop an effective B0AT1 inhibitor for phenylketonuria treatment.
  • Utilized structure-guided design to create inhibitors targeting dynamic allosteric sites.
  • Tested inhibitor effectiveness in a mouse model of phenylketonuria.
  • Demonstrated significant inhibition of B0AT1 activity in the mouse model.
  • Provided a framework for optimizing further B0AT1 inhibitors.

Abstract

AT1 and establish a framework for the rational optimization of inhibitors targeting conformationally dynamic allosteric sites in SLC6-family transporters.

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Cite This Study

Imazu et al. (2026) studied this question.

synapsesocial.com/papers/6a40b96161bb0a67205c59f5https://doi.org/10.1038/s42003-026-10535-y
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Molecular basis of inhibition of the amino acid transporter B0AT1 (SLC6A19)2024
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