Publications by authors named "Takato Mashita"

Artificial control of intracellular protein dynamics with high precision provides deep insight into complicated biomolecular networks. Optogenetics and caged compound-based chemically induced dimerization (CID) systems are emerging as tools for spatiotemporally regulating intracellular protein dynamics. However, both technologies face several challenges for accurate control such as the duration of activation, deactivation rate and repetition cycles.

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Selective inhibitors of dihydrofolate reductase (eDHFR) are crucial chemical biology tools that have widespread clinical applications. We developed a set of eDHFR-selective photoswitchable inhibitors by derivatizing the structure of our previously reported methotrexate (MTX) azolog, . Substitution of the skeletal -phenylene group of azoMTX with bulky bis-alkylated arylazopyrazole moieties significantly increased its selectivity toward eDHFR over human DHFR.

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Article Synopsis
  • Photopharmacology is emerging as a method to control biomolecules using light, inspired by caged compounds and optogenetics.
  • A new inhibitor, called azoMTX, was created by modifying methotrexate to enable it to switch between active and inactive forms when exposed to different wavelengths of light.
  • This innovative design allows for precise, real-time control of enzyme activity, offering a promising approach for studying and manipulating biological processes.
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