Light‐Wavelength‐Based Quantitative Control of Dihydrofolate Reductase Activity by Using a Photochromic Isostere of an Inhibitor
| العنوان: | Light‐Wavelength‐Based Quantitative Control of Dihydrofolate Reductase Activity by Using a Photochromic Isostere of an Inhibitor |
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| المؤلفون: | Toshiyuki Kowada, Takato Mashita, Toshitaka Matsui, Hiroto Takahashi, Shin Mizukami |
| المصدر: | ChemBioChem. 20:1382-1386 |
| بيانات النشر: | Wiley, 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Photoisomerization, Isostere, Molecular Conformation, Dihydrofolate reductase activity, Ligands, 010402 general chemistry, 01 natural sciences, Biochemistry, Enzyme catalysis, Photochromism, Dihydrofolate reductase, Escherichia coli, Molecular Biology, chemistry.chemical_classification, Binding Sites, biology, 010405 organic chemistry, Ligand, Biomolecule, Organic Chemistry, Combinatorial chemistry, 0104 chemical sciences, Kinetics, Tetrahydrofolate Dehydrogenase, Methotrexate, chemistry, biology.protein, Folic Acid Antagonists, Molecular Medicine |
| الوصف: | 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. |
| تدمد: | 1439-7633 1439-4227 |
| DOI: | 10.1002/cbic.201800816 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7045620ffd9bc1cff3b6e8211bc59248 https://doi.org/10.1002/cbic.201800816 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....7045620ffd9bc1cff3b6e8211bc59248 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14397633 14394227 |
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| DOI: | 10.1002/cbic.201800816 |