Phototrexate

Photopharmacological agent

trans-Phototrexate
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Phototrexate is a photopharmacological agent<ref name="VelemaSzymanski2014">,

 Photopharmacology: Beyond Proof of Principle, 
 Journal of the American Chemical Society, 
 2014,
 Vol. 136(Issue: 6),
 pp. 2178–2191,
 DOI: 10.1021/ja413063e,</ref><ref name="BroichhagenFrank2015">, 
 A Roadmap to Success in Photopharmacology, 
 Accounts of Chemical Research, 
 2015,
 Vol. 48(Issue: 7),
 pp. 1947–1960,
 DOI: 10.1021/acs.accounts.5b00129,</ref> that behaves as light-regulated inhibitor of the dihydrofolate reductase (DHFR).<ref name="MateraGomila2018">, 
 Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy, 
 Journal of the American Chemical Society, 
 2018,
 Vol. 140(Issue: 46),
 pp. 15764–15773,
 DOI: 10.1021/jacs.8b08249,</ref><ref name="MashitaKowada2019">, 
 Light‐Wavelength‐Based Quantitative Control of Dihydrofolate Reductase Activity by Using a Photochromic Isostere of an Inhibitor, 
 ChemBioChem, 
 2019,
 
 
 DOI: 10.1002/cbic.201800816,</ref> It is a photoisomerizable structural analogue of the chemotherapy agent methotrexate. Pharmacological effects of phototrexate can be switched on and off by UVA and visible light, respectively. Phototrexate is almost inactive in its trans configuration while it behaves as a potent antifolate in its cis configuration. It can also spontaneously self-deactivate in the dark.

cis-Phototrexate

See also

• Cancer
• Psoriasis
• Psoriatic arthritis

References

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