AI 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.
Article Abstract
Photopharmacology has attracted research attention as a new tool for achieving optical control of biomolecules, following the methods of caged compounds and optogenetics. We have developed an efficient photopharmacological inhibitor-azoMTX-for Escherichia coli dihydrofolate reductase (eDHFR) by replacing some atoms of the original ligand, methotrexate, to achieve photoisomerization properties. This fine molecular design enabled quick structural conversion between the active "bent" Z isomer of azoMTX and the inactive "extended" E isomer, and this property afforded quantitative control over the enzyme activity, depending on the wavelength of irradiating light applied. Real-time photoreversible control over enzyme activity was also achieved.
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| http://dx.doi.org/10.1002/cbic.201800816 | DOI Listing |
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